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  • Title: Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors.
    Author: Hu Q, Yin L, Jagusch C, Hille UE, Hartmann RW.
    Journal: J Med Chem; 2010 Jul 08; 53(13):5049-53. PubMed ID: 20550118.
    Abstract:
    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.
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