4.7 Article

Isopropylidene Substitution Increases Activity and Selectivity of Biphenylmethylene 4-Pyridine Type CYP17 Inhibitors

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 53, Issue 13, Pages 5049-5053

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jm100400a

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GYP 17 inhibition is a promising therapy for prostate cancer (PC) because proliferation of 80% of PC depends on androgen stimulation. Introduction of isopropylidene substituents onto the linker of biphenylmethylene 4-pyridines resulted in several strong GYP 17 inhibitors, which were more potent and selective, regarding GYP 11B1, 11B2, 19 and 3A4, than the drug candidate abiraterone.

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