3.1.4.1: phosphodiesterase I
This is an abbreviated version!
For detailed information about phosphodiesterase I, go to the full flat file.
Word Map on EC 3.1.4.1
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3.1.4.1
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camp
-
phosphodiesterases
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calcification
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arterial
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topoisomerase
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rolipram
-
monophosphate
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camp-specific
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infancy
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osteoblast
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hypophosphatemic
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rickets
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camptothecin
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pseudoxanthoma
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ectoenzyme
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topotecan
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5'-nucleotide
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elasticum
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ibmx
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ankylosis
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3'-phosphate
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zaprinast
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top1-dna
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camp-pde
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tcf7l2
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milrinone
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qq
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tissue-nonspecific
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cgmp-inhibited
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cgmp-stimulated
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pyrophosphohydrolase
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cilomilast
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cementum
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3-isobutyl-1-methylxanthine
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rolipram-sensitive
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vinpocetine
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cardiotonic
-
pharmacology
-
medicine
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synthesis
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drug development
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biotechnology
-
analysis
- 3.1.4.1
- camp
- phosphodiesterases
- calcification
- arterial
-
topoisomerase
- rolipram
- monophosphate
-
camp-specific
-
infancy
- osteoblast
-
hypophosphatemic
- rickets
- camptothecin
-
pseudoxanthoma
-
ectoenzyme
- topotecan
-
5'-nucleotide
- elasticum
- ibmx
- ankylosis
- 3'-phosphate
- zaprinast
-
top1-dna
- camp-pde
-
tcf7l2
- milrinone
-
tissue-nonspecific
-
cgmp-inhibited
-
cgmp-stimulated
-
pyrophosphohydrolase
- cilomilast
-
cementum
- 3-isobutyl-1-methylxanthine
-
rolipram-sensitive
- vinpocetine
-
cardiotonic
- pharmacology
- medicine
- synthesis
- drug development
- biotechnology
- analysis
Reaction
Synonyms
5' nucleotide phosphodiesterase/alkaline phosphodiesterase I, 5'-exonuclease, 5'-NPDase, 5'-nucleotide phosphodiesterase, 5'-PDase, 5'-PDE, 5'-phosphodiesterase, 5'NPDE, alkaline phosphodiesterase, Ap3A (Ap4A) hydrolase, autotaxin, B10, calcium-dependent phosphodiesterase 1C, cleavage/polyadenylation specificity factor, CPSF-73, cRNPMase-5'-PDase, cyclic nucleotide phosphodiesterase 1, cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase I, ecto-NPPase, ecto-nucleotide pyrophosphatase/phosphodiesterase 1, ectonucleotide pyrophosphatase phosphodiesterase 1, ectonucleotide pyrophosphatase/phosphodiesterase 1, ectonucleotide pyrophosphate/phosphodiesterase-1, ENPP-1, ENPP1, exonuclease I, exophosphodiesterase, gp130RB13-6, liver alkaline phosphodiesterase 1, liver nucleotide phosphodiesterase, More, NPP, NPP-1, NPP/PDE, NPP1, NPP2, NPP3, nucleotide phosphodiesterase, nucleotide phosphodiesterase/pyrophosphatase, nucleotide pyrophosphatase/alkaline phosphodiesterase I, nucleotide pyrophosphatase/phosphodiesterase 1, nucleotide pyrophosphatase/phosphodiesterase I, nucleotide pyrophosphatase/phosphodiesterase-1, nucleotide pyrophosphatase/phosphodiesterase-2, nucleotide pyrophosphatase/phosphodiesterase-3, orthophosphoric diester phosphohydrolase, PC-1, PDase, PDE, PDE 1A, PDE I, PDE1, PDE1A, PDE1C, PDE4A, PDEase, phosphodiesterase, phosphodiesterase 1, phosphodiesterase 1A, phosphodiesterase 1C, phosphonate monoester hydrolase/phosphodiesterase, phosphoric diester hydrolase, plant exonuclease I, plasma cell antigen 1, plasma cell membrane glycoprotein, plasma cell membrane protein-1, PMH, RNase J1, SMPDL3A, sphingomyelin phosphodiesterase, acid-like 3A, SVPD, Tdp 1, TDP1, tRNase Z, tyrosyl DNA phosphodiesterase 1, tyrosyl-DNA phosphodiesterase 1, tyrosyl-DNA phosphodiesterase I, tyrosyl-DNA-phosphodiesterase I, yfcE
ECTree
3.1.4.1 phosphodiesterase IAdvanced search results
results (
results (Inhibitors
Inhibitors on EC 3.1.4.1 - phosphodiesterase I
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INHIBITOR 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
(2R,4R,4aR,7R,8aS)-4,7-dimethyl-2-(5-aminothiophen-2-yl)octahydro-2H-chromen-4-ol
-
(2R,4S,4aR,7R,8aS)-4,7-dimethyl-2-(5-aminothiophen-2-yl)octahydro-2H-chromen-4-ol
-
(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]-isoquinolin-3-yl)carbamic acid
-
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(S)-3-(4-hydroxy-3-methoxyphenyl)propane-1,2-diol-2-beta-D-(6'-O-galloyl) glucopyranoside
-
1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10,12-dibromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10,12-dibromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10,12-dibromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10,12-dibromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10,12-dibromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10,12-dibromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10-bromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10-bromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10-bromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
11,13-dibromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
2,2,2-trifluoro-N-(5-((2R,4R,4aR,7R,8aR)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)acetamide
-
2,2,2-trifluoro-N-(5-((2R,4S,4aR,7R,8aR)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)acetamide
-
2,2,2-trifluoro-N-(8-(trifluoromethyl)benzo[f][1,2,3,4,5]pentathiepin-6-yl)acetamide
-
2-((6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino)acetic acid
-
-
2-(2,6-dimethylhept-5-en-1-yl)-5,7-dimethyl-1,3-diazatricyclo[3.3.1.1(3,7)]decan-6-one
-
2-(3-(dimethylamino)propoxy)-3-methoxy-6-(3-morpholinopropyl)-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
-
-
2-(3-(ethylamino)propoxy)-3-methoxy-6-(3-morpholinopropyl)-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
-
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2-(3-aminopropoxy)-3-methoxy-6-(3-morpholinopropyl)-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
-
-
2-(dibutylamino)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
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2-(piperidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
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2-(pyrrolidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
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2-morpholino-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
-
3-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
-
3-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
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3-((3,4,5-trimethoxybenzyl)oxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
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3-(2-((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)ethoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
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3-(4-hydroxy-3-methoxyphenyl)propane-1,2-diol 2-beta-D-(6'-O-galloyl)glucopyranoside
-
3-(4-methoxy-phenyl)-1-(3-nitro-phenyl)-8Hpyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
3-(piperidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide
-
3-(pyrrolidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide
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3-amino-6-(3-aminopropyl)-5,6-dihydro-9-methoxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline dihydrochloride
-
-
3-cyano-6,11-dihydro-5,11-dioxo-6-[3-(dimethylaminopropyl)-5H-indeno[1,2-c]isoquinoline]
-
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3-iodo-9-methoxy-6-(3-(dimethylamino)propyl)-5H-indeno-[1,2-c]isoquinoline-5,11(6H)-dione
-
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3-methoxy-6-(3-morpholinopropyl)-2-(3-(piperidin-1-yl)-propoxy)-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
-
-
3-methoxy-6-(3-morpholinopropyl)-2-(3-(pyrrolidin-1-yl)-propoxy)-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
-
-
3-morpholino-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide
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4-[(6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-4-oxobutanoic acid
-
-
6,6'-[(1R,2R,3S,4S)-2,4-bis(4-hydroxyphenyl)cyclobutane-1,3-diyl]di(2H-pyran-2-one)
-
6,6'-[propane-1,3-diylbis(iminopropane-3,1-diyl)]bis(5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione)
-
-
6-(3-(1H-imidazol-1-yl)propyl)-8-methoxy-3-nitro-5Hindeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(3-aminopropyl)-3-(methylamino)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(3-aminopropyl)-5,6-dihydro-8-methoxy-3-nitro-5,11-dioxo-11H-indeno[1,2-c]isoquinoline
-
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6-(3-aminopropyl)-5,6-dihydro-9-methoxy-3-iodo-5,11-dioxo-11H-indeno[1,2-c]isoquinoline
-
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6-(3-aminopropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
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6-(3-aminopropyl)-7-methoxy-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
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6-(3-aminopropyl)-8-hydroxy-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
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6-(3-aminopropyl)-9-methoxy-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
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6-[(6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-6-oxohexanoic acid
-
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7-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
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7-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-4-methyl-2H-chromen-2-one
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7-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
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7-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-4-methyl-2H-chromen-2-one
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7-((3,4,5-trimethoxybenzyl)oxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
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7-(2-((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)ethoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
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7-[[(1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl]methoxy]-2,3-dihydrobenzo[b]cyclopenta[d]pyran-4(1H)-one
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8-methoxymethyl isobutylmethylxanthine
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20 microM, 8-MM-IBMX, a selective PDE1 inhibitor, no effect on either JG cell cAMP content or renin release compared to untreated controls
9,11-dibromo-1-(2-furyl)-3-(4-tolyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
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9,11-dibromo-1-(4-chlorophenyl)-3-(4-tolyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
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9,11-dibromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
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9-bromo-1-(4-chlorophenyl)-3-(4-tolyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
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alpha,beta-methylene-adenosine triphosphate
-
inhibition in decreasing order: alpha,beta-methyl-adenosine triphosphate, ATP, UTP, GTP, CTP
CTP
-
inhibition in decreasing order: alpha,beta-methylene-adenosine triphosphate, ATP, UTP, GTP, CTP
diisopropyl fluorophosphate
-
bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
ethyl 2-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5Hindeno[1,2-c]isoquinolin-3-yl)amino]acetate
-
-
Fe2+
-
bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
Fe3+
-
bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase, 50% inhibition
IC86340
-
a PDE1 inhibitor, significantly reduces collagen I in human saphenous vein explants undergoing spontaneous remodeling via ex vivo culture, and acts synergistically with bicarbonate, in the absence of bicarbonate of IC86340, itself has no effect on collagen I protein. PDE1C but not PDE1A is the major isoform responsible for mediating the effects of IC86340. Lysosome inhibitors,. i.e. 2',4'-dichlorobenzamil, a nonselective CNG channel blocker, and the more specific CNG channel blocker, L-cisdiltiazem, block IC86340-mediated collagen I reduction, overview
-
isobutylmethylxanthine
-
100 microM, a nonselective PDE1 inhibitor, increases cAMP and renin relase by 72% and 118%, respectively
methyl 2-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5Hindeno[1,2-c]isoquinolin-3-yl)amino]-2-oxoacetate
-
-
methyl 3-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5Hindeno[1,2-c]isoquinolin-3-yl)amino]-3-oxopropanoate
-
-
methyl 4-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5Hindeno[1,2-c]isoquinolin-3-yl)amino]-4-oxobutanoate
-
-
methyl 5-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5Hindeno[1,2-c]isoquinolin-3-yl)amino]-5-oxopentanoate
-
-
methyl 6-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5Hindeno[1,2-c]isoquinolin-3-yl)amino]-6-oxohexanoate
-
-
methyl-3,4-dephostatin
a dephostatin derivative, structure-activity relationship analogues of this active compound that have a chemical substitution at a single position show a dramatic decrease in inhibition activity
N-(2-[1-[2-(2-methyl-1H-imidazol-1-yl)pyrimidin-4-yl]piperidin-4-yl]ethyl)sulfuric diamide
-
-
N-(2-[1-[6-(2-methyl-1H-imidazol-1-yl)pyrimidin-4-yl]piperidin-4-yl]ethyl)sulfuric diamide
-
-
N-(5-((2R,4R,4aR,7R,8aR)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)acetamide
-
N-(5-((2R,4R,4aR,7R,8aR)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)benzamide
-
N-(5-((2R,4R,4aR,7R,8aS)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)adamantane-1-carboxamide
-
N-(5-((2R,4S,4aR,7R,8aR)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)acetamide
-
N-(5-((2R,4S,4aR,7R,8aR)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2yl)benzamide
-
N-(5-((2R,4S,4aR,7R,8aS)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)adamantane-1-carboxamide
-
N-(6-Aminohexyl)-5-chloro-1-naphthalenesulfonamide
-
W7, 10 microM, a calcium-calmodulin inhibitor
N-[2-(1-[6,7-dimethoxy-2-[(E)-2-(pyridin-3-yl)ethenyl]quinazolin-4-yl]piperidin-4-yl)ethyl]sulfuric diamide
-
-
N-[2-[1-(2-ethyl-6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
-
-
N-[2-[1-(6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
-
enzyme binding, structure modelling, overview
N-[6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl]acetamide
-
-
N2,N2-dibutyl-N-[8-(trifluoromethyl)-1,2,3,4,5-benzopentathiepin-6-yl]glycinamide
-
phenylmethylsulfonyl fluoride
-
FS-44: 5'-PDase activity of bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
vinpocetin
-
10 mU, surpresses the increase of activity, caused by the addition of 0.2 mM Ca2+
1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
-
-
1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10,12-dibromo-1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10,12-dibromo-1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10,12-dibromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10,12-dibromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10,12-dibromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10,12-dibromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10,12-dibromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10,12-dibromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10,12-dibromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10,12-dibromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10,12-dibromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10,12-dibromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10,12-dibromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10,12-dibromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10-bromo-1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10-bromo-1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10-bromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10-bromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10-bromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10-bromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10-bromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10-bromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10-bromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10-bromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10-bromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10-bromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10-bromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10-bromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
11,13-dibromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
-
-
11,13-dibromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
11-bromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
-
-
11-bromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
9,11-dibromo-1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
9,11-dibromo-1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
-
9,11-dibromo-1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
9,11-dibromo-1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
-
9,11-dibromo-1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
9,11-dibromo-1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
-
9,11-dibromo-1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
9-bromo-1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
9-bromo-1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
-
9-bromo-1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
9-bromo-1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
-
9-bromo-1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
9-bromo-1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
-
9-bromo-1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
AMP
-
5'-AMP, but 2'-AMP, 3'-AMP, 3': 5'cAMP and 2': 3'cAMP has no inhibiting effects; competitive; product inhibition
ATP
-
inhibition in decreasing order: alpha,beta-methylene-adenosine triphosphate, ATP, UTP, GTP, CTP
Co2+
-
FS-44: 5'-PDase activity of bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
Cu2+
-
FS-44: 5'-PDase activity of bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
EDTA
-
PC-1, nucleotide pyrophosphatase/phosphodiesterase I: glycine-enhanced inhibition, reversed by Mg2+
EDTA
-
complete inhibition, addition of EDTA plus Ca2+ or Mn2+ results in partial inhibition
glycine
-
PC-1, nucleotide pyrophosphatase/phosphodiesterase I: at high concentrations, 100 mM; PC-1, nucleotide pyrophosphatase/phosphodiesterase I: glycine-enhanced inhibition by EDTA, by itself, up to 25 mM, is not inhibitory
glycine
-
liver, 0.1 M glycine, inhibition initially 20-30%, 90% inhibition obtained after 60 min preincubation
GTP
-
inhibition in decreasing order: alpha,beta-methylene-adenosine triphosphate, ATP, UTP, GTP, CTP
Hg2+
-
FS-44: 5'-PDase activity of bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
IBMX
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intra peritoneal to the rats
indomethacin
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
Mn2+
-
FS-44: 5'-PDase activity of bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
NSC88915
a deoxycorticosterone derivative of progesterone coupled to methyl-p-toluene-sulfonate, structure-activity relationship analogues of this active compound that have a chemical substitution at a single position show a dramatic decrease in inhibition activity
UTP
-
inhibition in decreasing order: alpha,beta-methylene-adenosine triphosphate, ATP, UTP, GTP, CTP
Zn2+
-
FS-44: 5'-PDase activity of bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
additional information
-
the enzyme is not inhibited by 5-[4-pyridyl]-1,3,4-oxadiazole-2(3H)-thione, 5-[3-benzyloxyphenyl]-1,3,4-oxadiazole-2(3H)-thione, 5-[4-benzyloxyphenyl]-3-octyl-1,3,4-oxadiazole-2(3H)-thione, 5-[4-benzyloxyphenyl]-3-benzyl-1,3,4-oxadiazole-2(3H)-thione, 5-[4-benzyloxyphenyl]-3-pentyl-1,3,4-oxadiazole-2(3H)-thione, 5-cyclohexyl-1,3,4-oxadiazole-2(3H)-thione, 5-diphenylmethyl-1,3,4-oxadiazole-2(3H)-thione, 5-[4-benzyloxyphenyl]-3-benzoyl-1,3,4-oxadiazole-2(3H)-thione, 5-[4-benzyloxyphenyl]-3-(2-hydroxyethyl)-1,3,4-oxadiazole-2(3H)-thione, 5-[1-naphthyl]-1,3,4-oxadiazole-2(3H)-thione, 5-phenyl-1,3,4-thiadiazole-2(3H)-thione, 5-[4-hydroxyphenyl]-3-benzyl-1,3,4-thiadiazole-2(3H)-thione, 5-[4-propoxyphenyl]-3-propyl-1,3,4-thiadiazole-2(3H)-thione, 5-diphenylmethyl-1,3,4-thiadiazole-2(3H)-thionr, 5-[4-hydroxyphenyl]-1,3,4-thiadiazole-2(3H)-thione, and 5-[4-benzyloxyphenyl]-3-benzyl-1,3,4-thiaadiazole-2(3H)-thione
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additional information
-
no inhibition by adenosine, inosine, phenylalanine and caffeine
-
additional information
-
not inhibitory: 3-isobutyl-1methylxanthine, Ro 20-1724, 13-dipropyl-8-p-sulfophenylxanthine
-
additional information
-
expression of PC-1 is down-regulated during adipocyte maturation
-
additional information
-
the enzyme is not inhibited by bis(1,3,4-oxadiazol-2-methyl)-5-thione, 5-[4-pyridyl]-1,3,4-oxadiazole-2(3H)-thione, 5-[3-hydroxyphenyl]-1,3,4-oxadiazole-2(3H)-thione, 5-[4-benzyloxyphenyl]-3-octyl-1,3,4-oxadiazole-2(3H)-thione, and 5-[4-(t-butyldimethylsilyloxy)-phenyl]-1,3,4-thiadiazole-2 (3H)-thione
-
additional information
-
design, synthesis, and evaluation of new indenoisoquinolines that are dual inhibitors of both tyrosyl-DNA phosphodiesterase I and topoisomerase 1, structure-activity relationships and cytotoxicity, overview. No inhibition by methyl 2-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-2-oxoacetate, methyl 3-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-3-oxopropanoate, methyl 4-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-4-oxobutanoate, methyl 5-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-5-oxopentanoate, methyl 6-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-6-oxohexanoate, 3-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]-isoquinolin-3-yl)amino]-3-oxopropanoic acid, methyl 3-[(6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-3-oxopropanoate, methyl 4-[(6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-4-oxobutanoate, methyl 5-[(6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-5-oxopentanoate, 5-[(6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-5-oxopentanoic acid, 2-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-2-oxoacetic acid, 3-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-3-oxopropanoic acid, 4-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-4-oxobutanoic acid, 5-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-5-oxopentanoic acid, 6-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-6-oxohexanoic acid, ethyl 2-[(6-Methyl-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]acetate, 2-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]-isoquinolin-3-yl)amino]acetic acid, 2-((6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino)acetic acid, 6-(3-bromopropyl)-5,6-dihydro-8-methoxy-3-nitro-5,11-dioxo-11H-indeno[1,2-c]isoquinoline, 6-(3-azidopropyl)-5,6-dihydro-8-methoxy-3-nitro-5,11-dioxo-11H-indeno[1,2-c]isoquinoline, 8-methoxy-6-(3-morpholinopropyl)-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione, N-[5,11-dioxo-6-[3-(2l5-triaz-1-en-2-yn-1-yl)propyl]-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl]acetamide, N-[6-(3-hydroxypropyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl]acetamide, N-[6-(3-aminopropyl)-11-hydroxy-5-oxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl]acetamide, 6-(3-hydroxypropyl)-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione, 3-cyano-5,11-dihydro-6-[3-(1H-imidazolyl)propyl]-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinoline, 3-cyano-6,11-dihydro-5,11-dioxo-6-(3-morpholinylpropyl)-5H-indeno[1,2-c]isoquinoline, and 3-cyano-5,11-dihydro-6-[3-(dimethylamino)propyl]-5,11-dioxoindeno[1,2-c]isquinoline. Molecular modeling of the enzyme based on crystal structure PDB 1RFF
-
additional information
docking simulations suggest that enzyme inhibitors bind within the catalytic pocket to prevent docking of endogenous substrates
-
additional information
-
synthesis and evaluation of dual tyrosyl-DNA phosphodiesterase I-topoisomerase I inhibitors based on the indenoisoquinoline chemotype, structure-activity relationship studies, overview
-
additional information
-
structure-based drug design, synthesis, and biological evaluation of O-2-modified indenoisoquinolines as dual topoisomerase I-tyrosyl-DNA phosphodiesterase I inhibitors, structure-activity relationships, molecular docking studies, and molecular modeling, overview. No inhibition by 2-(allyloxy)-3-methoxy-6-(3-morpholinopropyl)-5H-[1,3]-dioxolo[4',5':5,6]indeno [1,2-c]isoquinoline-5,12(6H)-dione, 3-methoxy-2-(3-morpholinopropoxy)-6-(3-morpholinopropyl)-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione, 3-methoxy-2-(3-(4-methylpiperazin-1-yl)propoxy)-6-(3-morpholinopropyl)-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]-isoquinoline-5,12(6H)-dione, methyl 2-((3-methoxy-6-(3-morpholinopropyl)-5,12-dioxo-6,12-dihydro-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]-isoquinolin-2-yl)oxy)acetate, and 2-((12-hydroxy-3-methoxy-6-(3-morpholinopropyl)-5-oxo-6,12-dihydro-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]-isoquinolin-2-yl)oxy)acetohydrazide. Antiproliferative potencies of selected O-2-modified indenoisoquinolines, overview
-
additional information
-
design and synthesis of highly potent and selective ectonucleotide pyrophosphatase/phosphodiesterase I inhibitors based on an adenosine 5-(alpha or gamma)-thio-(alpha,beta- or beta,gamma)-methylenetriphosphate scaffold, compound configurations analsis by NMR spectroscopy, overview. Analogue 4 is not a good inhibitor. The thiophosphate groups are designed to chelate the tentative Zn2+ ions. Docking od 1-3 into the NPP1 model suggests that activity correlates with the number of H-bonds with binding site residues, overview
-
additional information
-
no inhibition by divalent cations, Mg2+ and Ca2+ , or p-chloromercuribenzoate
-
additional information
PC-1 promoter activity induced by osteoblast differentiation is inhibited by fibroblast growth factor 2
-
additional information
-
not inhibitory: ouabain, N-ethylmaleimide, levamisole, sodium azide
-
additional information
-
not inhibitory to renal ecto-phosphodiesterase: 8-methoxymethyl-3-isobutyl-1-methylxanthine, erythro-9-(2-hydroxy-3-nonyl)adenine, milrinone, cGMP, 4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one, zaprinast, 5-nitro-2,N,N-trimethylbenzenesulfonamide
-
additional information
-
not inhibitory: levamisole, sodium azide, gadolinium chloride
-
additional information
-
synthesis of 1,2,9,11-tetrasubstituted 7H-thieno[2',3':4,5]pyrimido[6,1-b]-quinazolin-7-one and 1,3,10,12-tetrasubstituted 8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one inhibitors, synthesis and evaluation, overview
-
additional information
-
bicarbonate acts synergistically with inhibitor IC86340
-
