{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Sammeta VR"],"funding":["U.S. Department of Energy","Susan G. Komen","U.S. Department of Defense","North Carolina Biotechnology Center"],"pagination":["1151-1158"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC9290010"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["13(7)"],"pubmed_abstract":["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."],"journal":["ACS medicinal chemistry letters"],"pubmed_title":["A New Chemotype of Chemically Tractable Nonsteroidal Estrogens Based on a Thieno[2,3-d]pyrimidine Core."],"pmcid":["PMC9290010"],"funding_grant_id":["CCR 19608597","BC170954","DE-AC02-06CH11257","2018-IDG-1030"],"pubmed_authors":["Fanning SW","McDonnell DP","Sammeta VR","Norris JD","Artham S","Willson TM","Byemerwa J","Torrice CD","Joiner C"],"additional_accession":[]},"is_claimable":false,"name":"A New Chemotype of Chemically Tractable Nonsteroidal Estrogens Based on a Thieno[2,3-d]pyrimidine Core.","description":"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.","dates":{"release":"2022-01-01T00:00:00Z","publication":"2022 Jul","modification":"2026-05-28T01:28:28.427Z","creation":"2024-11-21T05:43:27.093Z"},"accession":"S-EPMC9290010","cross_references":{"pubmed":["35859859"],"doi":["10.1021/acsmedchemlett.2c00180"]}}