Synthesis of 2-Phenylbenzofuran Derivatives as Testosterone 5. ALPHA.-Reductase Inhibitor.

…, M Sugiyama, T Hamada, H Horikoshi, T Nishi

Index: Ishibashi, Koki; Nakajima, Katsuyoshi; Sugioka, Yuki; Sugiyama, Mitsuo; Hamada, Takakazu; Horikoshi, Hiroyoshi; Nishi, Takahide Chemical and Pharmaceutical Bulletin, 1999 , vol. 47, # 2 p. 226 - 240

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Citation Number: 12

Abstract

A series of 2-phenylbenzofuran derivatives with a carbamoyl, alkylamino, or alkyloxy group at the 5 or 6 position of the benzofuran ring were synthesized and evaluated for rat and human testosterone 5α-reductase inhibitory activities in vitro. Against rat enzyme, the carbamoyl derivatives had more potent inhibitory activities than the alkylamino or alkyloxy derivatives, and the 6-carbamoyl derivatives tended to be more potent than the 5- ...

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