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Literature summary for 1.14.14.19 extracted from

  • Pinto-Bazurco Mendieta, M.; Negri, M.; Hu, Q.; Hille, U.; Jagusch, C.; Jahn-Hoffmann, K.; Mueller-Vieira, U.; Schmidt, D.; Lauterbach, T.; Hartmann, R.
    CYP17 inhibitors. Annulations of additional rings in methylene imidazole substituted biphenyls: Synthesis, biological evaluation and molecular modelling (2008), Arch. Pharm., 341, 547-609.
    View publication on PubMed
Search for more literature for 1.14.14.19

Application

Application Comment Organism
drug development the enzyme is a target for inhibitor design Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
CYP17, expression in Escherichia coli, co-expression with NADPH-P450 reductase Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(4-(benzo[b]thiophen-5-yl)phenyl)methanol 2% inhibition at 200 nM and 39% inhibition at 0.002 mM Homo sapiens
1-((4-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)phenyl)-methyl)-1H-imidazole 19% inhibition at 200 nM and 74% inhibition at 0.002 mM Homo sapiens
1-(1-(4-(benzo[b]thiophen-5-yl)phenyl)propyl)-1H-imidazole 21% inhibition at 200 nM and 75% inhibition at 0.002 mM Homo sapiens
1-(1-(4-(naphthalen-2-yl)phenyl)propyl)-1H-imidazole
-
 Homo sapiens
1-(3-(4-(6-(tert-butyldimethylsilyloxy)naphthalen-2-yl)phenyl)pentan-3-yl)-1H-imidazole
-
 Homo sapiens
1-(4-(6-methoxynaphthalen-2-yl)phenyl)propan-1-ol 7% inhibition at 200 nM and 43% inhibition at 0.002 mM Homo sapiens
1-(4-(benzofuran-5-yl)benzyl)-1H-imidazole no inhibition at 200 nM and 21% inhibition at 0.002 mM Homo sapiens
4-(8-(1-(1H-imidazol-1-yl)propyl)quinolin-5-yl)phenol 17% inhibition at 200 nM and 71% inhibition at 0.002 mM Homo sapiens
4-(benzo[b]thiophen-5-yl)benzaldehyde 7% inhibition at 200 nM and 40% inhibition at 0.002 mM Homo sapiens
5-(4-(1-(1H-imidazol-1-yl)propyl)phenyl)-1H-indole 5% inhibition at 200 nM and 27% inhibition at 0.002 mM Homo sapiens
5-(4-(1H-imidazol-1-ylmethyl)phenyl)-1H-indole 5% inhibition at 200 nM and 39% inhibition at 0.002 mM Homo sapiens
6-(4-(1H-imidazol-1-ylmethyl)phenyl)benzo[d]thiazole no inhibition at 200 nM and 17% inhibition at 0.002 mM Homo sapiens
6-(4-(3-(1H-imidazol-1-yl)pentan-3-yl)phenyl)naphthalen-2-ol 16% inhibition at 200 nM and 74% inhibition at 0.002 mM Homo sapiens
abiraterone
-
 Homo sapiens
ketoconazole is a weak inhibitor of CYP17, 29% inhibition at 0.0002 mM Homo sapiens
additional information CYP17 inhibitory activities, docking and molecular modelling of inhibitors, overview Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
17alpha-hydroxylase-17,20-lyase
-
 Homo sapiens
CYP17
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.667
-
-
 Homo sapiens 1-(1-(4-(benzo[b]thiophen-5-yl)phenyl)propyl)-1H-imidazole

General Information

General Information Comment Organism
metabolism CYP17 is the key enzyme for the biosynthesis of androgens Homo sapiens