A New Chemotype of Chemically Tractable Nonsteroidal Estrogens Based on a Thieno[2,3-d]pyrimidine Core.

Journal Article (Journal Article)

Despite continued interest in the development of nonsteroidal estrogens and antiestrogens, there are only a few chemotypes of estrogen receptor ligands. Using targeted screening in a ligand sensing assay, we identified a phenolic thieno[2,3-d]pyrimidine with affinity for estrogen receptor α. An efficient three-step synthesis of the heterocyclic core and structure-guided optimization of the substituents resulted in a series of potent nonsteroidal estrogens. The chemical tractability of the thieno[2,3-d]pyrimidine chemotype will support the design of new estrogen receptor ligands as therapeutic hormones and antihormones.

Full Text

Duke Authors

Cited Authors

  • Sammeta, VR; Norris, JD; Artham, S; Torrice, CD; Byemerwa, J; Joiner, C; Fanning, SW; McDonnell, DP; Willson, TM

Published Date

  • July 14, 2022

Published In

Volume / Issue

  • 13 / 7

Start / End Page

  • 1151 - 1158

PubMed ID

  • 35859859

Pubmed Central ID

  • PMC9290010

International Standard Serial Number (ISSN)

  • 1948-5875

Digital Object Identifier (DOI)

  • 10.1021/acsmedchemlett.2c00180

Language

  • eng

Conference Location

  • United States