Estrogen receptor ligands. Part 7: Dihydrobenzoxathiin SERAMs with bicyclic amine side chains

Timothy A Blizzard; Frank DiNinno; Jerry D Morgan 2nd; Helen Y Chen; Jane Y Wu; Candido Gude; Seongkon Kim; Wanda Chan; Elizabeth T Birzin; Yi Tien Yang; Lee-Yuh Pai; Zhoupeng Zhang; Edward C Hayes; Carolyn A DaSilva; Wei Tang; Susan P Rohrer; James M Schaeffer; Milton L Hammond

doi:10.1016/j.bmcl.2004.05.074

Estrogen receptor ligands. Part 7: Dihydrobenzoxathiin SERAMs with bicyclic amine side chains

Bioorg Med Chem Lett. 2004 Aug 2;14(15):3861-4. doi: 10.1016/j.bmcl.2004.05.074.

Authors

Timothy A Blizzard¹, Frank DiNinno, Jerry D Morgan 2nd, Helen Y Chen, Jane Y Wu, Candido Gude, Seongkon Kim, Wanda Chan, Elizabeth T Birzin, Yi Tien Yang, Lee-Yuh Pai, Zhoupeng Zhang, Edward C Hayes, Carolyn A DaSilva, Wei Tang, Susan P Rohrer, James M Schaeffer, Milton L Hammond

Affiliation

¹ Merck Research Laboratories, Medicinal Chemistry, RY800-B116, PO Box 2000, Rahway, NJ 07065, USA. tim_blizzard@merck.com

PMID: 15225685
DOI: 10.1016/j.bmcl.2004.05.074

Abstract

A series of benzoxathiin SERAMs with bicyclic amine side chains was prepared. Minor modifications in the side chain resulted in significant effects on biological activity, especially in uterine tissue.

MeSH terms

Animals
Bridged Bicyclo Compounds / chemistry*
Bridged Bicyclo Compounds / pharmacology
Female
Kinetics
Ligands*
Models, Molecular
Molecular Conformation
Receptors, Estrogen / metabolism*
Selective Estrogen Receptor Modulators / chemistry
Selective Estrogen Receptor Modulators / metabolism*
Selective Estrogen Receptor Modulators / pharmacology
Structure-Activity Relationship
Uterus / drug effects

Substances

Bridged Bicyclo Compounds
Ligands
Receptors, Estrogen
Selective Estrogen Receptor Modulators