|
|||||
|
|
Lead identification of a potent benzopyranone selective estrogen receptor modulator |
|
| Authors: | McKie Jeffrey A Bhagwat Shripad S Brady Helen Doubleday Mary Gayo Leah Hickman Mathew Jalluri Ravi K Khammungkhune Sak Kois Adam Mortensen Deborah Richard Normand Sapienza John Shevlin Graziella Stein Bernd Sutherland May |
| Affiliation: | Medicinal Chemistry, Celgene, San Diego, CA 92121, USA. jmckie@celgene.com |
| Abstract: | Starting from a phenol screening hit (6), three series of benzopyranone selective estrogen receptor modulators (SERMs) have been designed, synthesized, and analyzed for both estrogen receptor alpha binding affinity and in vitro activity in two cell assays. The lead compound identified, SP500263 (13), was more potent than raloxifene and tamoxifen in a cell-based assay measuring inhibition of interleukin-6 release. |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ | |