Benzothieno[3,2-b]indole derivatives as potent selective estrogen receptor modulators

Qinggang Ji; Jie Gao; Junbo Wang; Chunhao Yang; Xin Hui; Xueming Yan; Xihan Wu; Yuyuan Xie; Ming-Wei Wang

doi:10.1016/j.bmcl.2005.03.111

Benzothieno[3,2-b]indole derivatives as potent selective estrogen receptor modulators

Bioorg Med Chem Lett. 2005 Jun 2;15(11):2891-3. doi: 10.1016/j.bmcl.2005.03.111.

Authors

Qinggang Ji¹, Jie Gao, Junbo Wang, Chunhao Yang, Xin Hui, Xueming Yan, Xihan Wu, Yuyuan Xie, Ming-Wei Wang

Affiliation

¹ State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Sciences, Graduate School of the Chinese Academy of Sciences.

PMID: 15911274
DOI: 10.1016/j.bmcl.2005.03.111

Abstract

A series of estrogen receptor ligands based on benzothieno[3,2-b]indole were synthesized and their binding affinity for estrogen receptor subtypes (ERalpha and ERbeta) and effects on mouse uterus and bone were evaluated. Some of these compounds showed strong binding affinity to ER and significantly increased the bone mineral density of ovariectomized mice.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Female
Humans
Indoles / pharmacology*
Mice
Selective Estrogen Receptor Modulators / chemistry
Selective Estrogen Receptor Modulators / pharmacology*

Substances

Indoles
Selective Estrogen Receptor Modulators