Reversible Inhibition of Human Placental Microsomal Aromatase by CGS 18320B and Other Non-Steroidal Compounds
- 1 January 1990
- journal article
- research article
- Published by Taylor & Francis in Endocrine Research
- Vol. 16 (2) , 255-267
- https://doi.org/10.1080/07435809009033004
Abstract
The effect of bis-(p-cyanophenyl)imidazo-1-yl-methane hemisuccinate (CGS 18320B) and other non-steroidal compounds on the aromatization of androstenedione by human placental microsomal aromatase was studied. CGS 18320B exhibited competitive inhibition with an apparent Ki of 0.16 nM, a 90 and 3800-fold increase in affinity compared to 4-hydroxyandrostenedione and aminoglutethimide, respectively. The inhibition is not time-dependent, indicating that the active site interaction is reversible. CGS 18230B showed a two-fold increased affinity as compared to 4-(5,6,7,8-tetrahydroimidazo[1,5a]pyridin-5-yl)benzonitrile (CGS 16949A) and cis-1-[(4-{(1-imidazoyl)methyl}cyclohexyl)methyl]-imidazole succinate (CGS 14796C) which showed Ki values of 0.35 and 0.39 4M, respectively. 1-[2-{1-(4-carboxyphenyl)-3-ureido}ethyl]-2-(4-pyridyl)-2-imidazoline monohydrochloride (CGP 15720A) showed negligible inhibition.This publication has 22 references indexed in Scilit:
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