Topic
Plomestane
About: Plomestane is a research topic. Over the lifetime, 2 publications have been published within this topic receiving 30 citations. The topic is also known as: propargylestrenedione & PED.
Papers
TL;DR: Biosynthetic CYP450 enzymes of those steroids that mediate specific disease processes are potential therapeutic targets for selective intervention by the design of specific pseudo-substrate analogs that will be activated during enzyme-directed catalysis to produce a reactive functional group in the enzyme's active site that will either tightly or irreversibly bind and inactivate the host enzyme.
24 citations
Journal Article•
TL;DR: The inhibition of human placental aromatase was used to rank a series of compounds, with the objective of selecting compounds for further evaluation as chemopreventive agents.
Abstract: The inhibition of human placental aromatase was used to rank a series of compounds, with the objective of selecting compounds for further evaluation as chemopreventive agents. (+/-)-p-Aminoglutethimide, introduced over two decades ago as a treatment for breast cancer, had an IC50 of 6.5 microM. Five compounds were more potent than aminoglutethimide in this assay: (+)- vorozole, 4-hydroxyandrostenedione, miconazole nitrate, plomestane, and 4-methoxy-androst-4-ene-3,17-dione. Other compounds with known chemoprevention activity, such as curcumin and genistein, were inactive. This assay for aromatase inhibitors is a rapid, economical way of ranking compounds for further development as chemoprevention agents.
8 citations
Performance Metrics
| Year | Papers |
|---|---|
| 1999 | 1 |
| 1995 | 1 |