| Literature DB >> 16806917 |
Yoshitake Kanbe1, Myung-Hwa Kim, Masahiro Nishimoto, Yoshihito Ohtake, Takaaki Yoneya, Iwao Ohizumi, Toshiaki Tsunenari, Kenji Taniguchi, Shin-ichi Kaiho, Yoshiaki Nabuchi, Hiroshi Araya, Setsu Kawata, Kazumi Morikawa, Jae-Chon Jo, Hee-An Kwon, Hyun-Suk Lim, Hak-Yeop Kim.
Abstract
In order to develop orally active pure antiestrogens, we incorporated the carboxy-containing side chains into the 7alpha-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.Entities:
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Year: 2006 PMID： 16806917 DOI： 10.1016/j.bmcl.2006.06.047
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823