-transparent.png){kind=logo}
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 5 alpha-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.
K Ishibashi, and
K Nakajima, and
Y Sugioka, and
M Sugiyama, and
T Hamada, and
H Horikoshi, and
T Nishi
December 1990,
The Journal of antibiotics,
K Ishibashi, and
K Nakajima, and
Y Sugioka, and
M Sugiyama, and
T Hamada, and
H Horikoshi, and
T Nishi
May 2003,
Planta medica,
K Ishibashi, and
K Nakajima, and
Y Sugioka, and
M Sugiyama, and
T Hamada, and
H Horikoshi, and
T Nishi
May 2016,
Bioorganic & medicinal chemistry letters,
K Ishibashi, and
K Nakajima, and
Y Sugioka, and
M Sugiyama, and
T Hamada, and
H Horikoshi, and
T Nishi
March 1992,
The Journal of steroid biochemistry and molecular biology,
K Ishibashi, and
K Nakajima, and
Y Sugioka, and
M Sugiyama, and
T Hamada, and
H Horikoshi, and
T Nishi
June 1985,
Journal of medicinal chemistry,
K Ishibashi, and
K Nakajima, and
Y Sugioka, and
M Sugiyama, and
T Hamada, and
H Horikoshi, and
T Nishi
February 1994,
The Journal of steroid biochemistry and molecular biology,
K Ishibashi, and
K Nakajima, and
Y Sugioka, and
M Sugiyama, and
T Hamada, and
H Horikoshi, and
T Nishi
May 1994,
Journal of immunoassay,
K Ishibashi, and
K Nakajima, and
Y Sugioka, and
M Sugiyama, and
T Hamada, and
H Horikoshi, and
T Nishi
December 1984,
Acta endocrinologica,
K Ishibashi, and
K Nakajima, and
Y Sugioka, and
M Sugiyama, and
T Hamada, and
H Horikoshi, and
T Nishi
March 2019,
Bioorganic chemistry,
K Ishibashi, and
K Nakajima, and
Y Sugioka, and
M Sugiyama, and
T Hamada, and
H Horikoshi, and
T Nishi
January 2012,
Chemical & pharmaceutical bulletin,
