17-Imidazolyl, Pyrazolyl, and Isoxazolyl Androstene Derivatives. Novel Steroidal Inhibitors of Human Cytochrome Cl7, 20-Lyase (P45017α)

…, J Li, Y Liu, K Kato, GT Klus, A Brodie

Index: Ling, Yang-Zhi; Li, Ji-Song; Liu, Yang; Kato, Katsuya; Klus, Gregory T.; Brodie, Angela Journal of Medicinal Chemistry, 1997 , vol. 40, # 20 p. 3297 - 3304

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Citation Number: 103

Abstract

We recently described a number of inhibitors of P45017α, the key enzyme of androgen biosynthesis. Here, we report the synthesis and activity of novel 17-imidazolyl, pyrazolyl, and isoxazolyl androstene derivatives as potential agents for the treatment of prostatic cancer. A number of 17-(4'-Imidazolyl) derivatives were prepared by condensing the corresponding 17- ketol acetate side chain with aldehyde and ammonium hydroxide. The 17β-(4'-imidazolyl) ...