Chemical and Pharmaceutical Bulletin p. 226 - 240 (1999)
Update date:2022-09-26
Topics:
Ishibashi, Koki
Nakajima, Katsuyoshi
Sugioka, Yuki
Sugiyama, Mitsuo
Hamada, Takakazu
Horikoshi, Hiroyoshi
Nishi, Takahide
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-carbamoyl derivatives. Against human enzyme, the 6-substituted derivatives had more potent inhibitory activities than the 5-substituted derivatives. The 6-carbamoyl and 6-alkylamino derivatives tended to show stronger inhibitory activities against human type 1 enzyme than against type 2 enzyme, but they were not largely selective.
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Doi:10.1016/S0040-4039(99)00215-4
(1999)Doi:10.1021/jo020423e
(2003)Doi:10.1016/S0040-4020(99)00038-1
(1999)Doi:10.1016/S0040-4020(99)00109-X
(1999)Doi:10.1016/S0040-4020(99)00069-1
(1999)Doi:10.1039/jr9460000776
(1946)
