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苯基硒取代甾体激素的合成与生化筛选

Synthesis and biochemical screening of phenylselenium-substituted steroid hormones.

作者信息

Konopelski J P, Djerassi C, Raynaud J P

出版信息

J Med Chem. 1980 Jul;23(7):722-6. doi: 10.1021/jm00181a004.

DOI:10.1021/jm00181a004
PMID:7401101
Abstract

The syntheses of phenylselenium-substituted progesterone [21- (1) and 17 alpha-(phenylseleno)progesterone (2)] and testosterone [16 beta- (3) and 16 alpha-(phenylseleno)testosterone (4)] derivatives are described, along with data which help to establish the stereochemistry of the substituents in the testosterone molecules. Except for 21-(phenylseleno)-progesterone, the molecules exhibit greatly reduced receptor-binding capabilities.

摘要

描述了苯基硒取代的孕酮[21-(1)和17α-(苯基硒基)孕酮(2)]以及睾酮[16β-(3)和16α-(苯基硒基)睾酮(4)]衍生物的合成,以及有助于确定睾酮分子中取代基立体化学的数据。除了21-(苯基硒基)-孕酮外,这些分子的受体结合能力大大降低。

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