Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer

Q Hu, C Jagusch, UE Hille, J Haupenthal…

Index: Hu, Qingzhong; Jagusch, Carsten; Hille, Ulrike E.; Haupenthal, Joerg; Hartmann, Rolf W. Journal of Medicinal Chemistry, 2010 , vol. 53, # 15 p. 5749 - 5758

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Citation Number: 42

Abstract

Androgens are well-known to stimulate prostate cancer (PC) growth. Thus, blockade of androgen production in testes and adrenals by CYP17 inhibition is a promising strategy for the treatment of PC. Moreover, many PC patients suffer from glucocorticoid overproduction, and importantly mutated androgen receptors can be stimulated by glucocorticoids. In this study, the first dual inhibitor of CYP17 and CYP11B1 (the enzyme responsible for the last ...