Author/Authors :
Yoshitake Kanbe، نويسنده , , Myung-Hwa Kim، نويسنده , , Masahiro Nishimoto، نويسنده , , Yoshihito Ohtake، نويسنده , , Takaaki Yoneya، نويسنده , , Iwao Ohizumi، نويسنده , , Toshiaki Tsunenari، نويسنده , , Kenji Taniguchi and Kenichi Nakashi ، نويسنده , , Shin-ichi Kaiho، نويسنده , , Yoshiaki Nabuchi، نويسنده , , Hiroshi Araya، نويسنده , , Setsu Kawata، نويسنده , , Kazumi Morikawa، نويسنده , , Jae-Chon Jo، نويسنده , , Hee-An Kwon، نويسنده , , Hyun-Suk Lim، نويسنده , , Hak-Yeop Kim، نويسنده ,
Abstract :
In order to develop orally active pure antiestrogens, we incorporated the carboxy-containing side chains into the 7α-position of the steroid scaffold and found that 17-keto derivative CH4893237 (12b) functioned as a pure antiestrogen with its oral activity much superior to clinically used pure antiestrogen, ICI182,780. Results from the pharmacokinetic evaluation indicated that the potent antiestrogen activity at oral dosing in mice attributed to both improved absorption from the intestinal wall and metabolic stability in liver.
Keywords :
Steroid scaffold , Carboxy moiety , estrogen receptor , Pure antiestrogen
