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

CYP17 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 CYP17 inhibitors, which were more potent and se...

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Veröffentlicht in:Journal of medicinal chemistry 2010-07, Vol.53 (13), p.5049-5053
Hauptverfasser: Hu, Qingzhong, Yin, Lina, Jagusch, Carsten, Hille, Ulrike E, Hartmann, Rolf W
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Sprache:eng
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Zusammenfassung:CYP17 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 CYP17 inhibitors, which were more potent and selective, regarding CYP 11B1, 11B2, 19 and 3A4, than the drug candidate abiraterone.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm100400a