Estrogen receptor ligands. Part 8: Dihydrobenzoxathiin SERAMs with heteroatom-substituted side chains

Timothy A Blizzard; Frank DiNinno; Jerry D Morgan 2nd; Jane Y Wu; Helen Y Chen; 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.2004.05.073

Estrogen receptor ligands. Part 8: Dihydrobenzoxathiin SERAMs with heteroatom-substituted side chains

Bioorg Med Chem Lett. 2004 Aug 2;14(15):3865-8. doi: 10.1016/j.bmcl.2004.05.073.

Authors

Timothy A Blizzard¹, Frank DiNinno, Jerry D Morgan 2nd, Jane Y Wu, Helen Y Chen, 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: 15225686
DOI: 10.1016/j.bmcl.2004.05.073

Abstract

A series of benzoxathiin SERAMs with heteroatom-substituted 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
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

Ligands
Receptors, Estrogen
Selective Estrogen Receptor Modulators