N??(4??Biphenylmethyl) imidazoles as Potential Therapeutics for the Treatment of Prostate Cancer: Metabolic Robustness Due to Fluorine Substitution?

F Leroux, TU Hutschenreuter, C Charrière…

Index: Leroux, Frederic; Hutschenreuter, Tilman U.; Charriere, Celine; Scopelliti, Rosario; Hartmann, Rolf W. Helvetica Chimica Acta, 2003 , vol. 86, # 7 p. 2671 - 2686

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Citation Number: 44

Abstract

Abstract 3, 3′, 5, 5′-And 2, 2′, 6, 6′-tetrafluoro-substituted 1-[(1, 1′-biphenyl]-4-yl) methyl]-1H-imidazoles were synthesized as inhibitors of 17α-hydroxylase-C17, 20-lyase (P450 17, CYP 17). P450 17 is the key enzyme of androgen biosynthesis. Its inhibition is a novel therapeutic approach for treatment of prostate cancer. To increase the so-far insufficient in vivo lifetime of such compounds, the metabolically sensitive positions were ...