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Literature summary for 5.6.2.1 extracted from

  • Cinelli, M.A.; Morrell, A.; Dexheimer, T.S.; Scher, E.S.; Pommier, Y.; Cushman, M.
    Design, synthesis, and biological evaluation of 14-substituted aromathecins as topoisomerase I inhibitors (2008), J. Med. Chem., 51, 4609-4619.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
14-(1-imidazolylmethyl)-2H-5,11a-diazadibenzo[b,h]fluoren-11-one
-
Homo sapiens
14-(1-morpholinomethyl)-2H-5,11a-diazadibenzo[b,h]fluoren-11-one
-
Homo sapiens
14-(3-aminopropyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one dihydrochloride
-
Homo sapiens
14-(3-N-ethanolaminopropyl)-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trifluoroacetate
-
Homo sapiens
14-(N,N-dimethylaminomethyl)-2H-5,11a-diazadibenzo[b,h]fluoren-11-one
-
Homo sapiens
14-(N-ethanolaminomethyl)-2H-5,11a-diazadibenzo[b,h]fluoren-11one
-
Homo sapiens
14-aminomethyl-12H-5,11a-diazadibenzo[b,h]fluoren-11-one dihydrochloride
-
Homo sapiens
14-chloromethyl-12H-5,11a-diazadibenzo[b,h]fluoren-11-one
-
Homo sapiens
14-[(1-imidazolyl)propylaminomethyl]-12H-5,11a-diazadibenzo[b,h]fluoren-11-one
-
Homo sapiens
14-[1-(N-methylpiperazinylmethyl)]-2H-5,11a-diazadibenzo[b,h]fluoren-11-one
-
Homo sapiens
14-[3(1-morpholinopropyl)]-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trifluoroacetate
-
Homo sapiens
14-[3-(1-imidazolylpropyl)]-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trifluoroacetate
-
Homo sapiens
14-[3-(N,N-dimethylaminopropyl)]-12H-5,11a-diazadibenzo[b,h]fluoren-11-one trifluoroacetate
-
Homo sapiens
14-[N-(S)-3-hydroxypyrrolidinomethyl]-12H-5,11a diazadibenzo[b,h]fluoren-11-one
-
Homo sapiens
22-hydroxyacuminatine
-
Homo sapiens
camptothecin
-
Homo sapiens
dimethoxyaromathecin
-
Homo sapiens
indenoisoquinoline
-
Homo sapiens
NSC 314622
-
Homo sapiens
rosettacin
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P11387
-
-

Source Tissue

Source Tissue Comment Organism Textmining
DU-145 cell human prostate tumor cell Homo sapiens
-
HCT-116 cell human colon tumor cell Homo sapiens
-
HOP-62 cell human lung tumor cell Homo sapiens
-
MDA-MB-435 cell MDA-MB-435MGM cell Homo sapiens
-
additional information each inhibitor compound is evaluated against approximately 60 cell lines originating from various human tumors Homo sapiens
-
OVCAR-3 cell human ovarian tumor cell Homo sapiens
-
SF-539 cell human CNS tumor cell Homo sapiens
-
SN-12C cell human renal tumor cell Homo sapiens
-
UACC-62 cell human melanoma tumor cell Homo sapiens
-

Synonyms

Synonyms Comment Organism
Top1
-
Homo sapiens
Topoisomerase I
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
GI50 values (the concentrations corresponding to 50% growth inhibition) for the different inhibitors with the different cell lines listed Homo sapiens additional information