ArticleJournal of medicinal chemistry2026
Development of a Second-Generation RARα Selective Antagonist as an Orally Bioavailable, Effective, Safe, and Reversible Male Contraceptive.
Rui Shi, Kristen John, Xuan Qin, Ehfazul Haque, Taimeng Liang, Narsihmulu Cheryala, Feng Li, Henry L Wong, Gunda I Georg
Abstract read
In one paragraphArticle in Journal of medicinal chemistry, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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2 · The registryThe trial behind it
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5 · Who and what moneyAuthors and funding
9 authors.
Rui ShiDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street SE, Minneapolis, Minnesota 55414, United States.
Kristen JohnDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street SE, Minneapolis, Minnesota 55414, United States.ORCID 0000-0002-9981-6100 Xuan QinCenter for Drug Discovery, Department of Pathology and Immunology, NMR and Drug Metabolism Core, Advanced Technology Cores, Department of Biochemistry and Molecular Pharmacology, Baylor College of Medicine, One Baylor Plaza, MS: BCM330, Houston, Texas 77030, United States.ORCID 0000-0003-3728-5911 Ehfazul HaqueDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street SE, Minneapolis, Minnesota 55414, United States.
Taimeng LiangDepartment of Chemistry, University of Minnesota, 207 Pleasant Street, SE, Minneapolis, Minnesota 55455-0431, United States.
Narsihmulu CheryalaDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street SE, Minneapolis, Minnesota 55414, United States.
Feng LiCenter for Drug Discovery, Department of Pathology and Immunology, NMR and Drug Metabolism Core, Advanced Technology Cores, Department of Biochemistry and Molecular Pharmacology, Baylor College of Medicine, One Baylor Plaza, MS: BCM330, Houston, Texas 77030, United States.
Henry L WongDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street SE, Minneapolis, Minnesota 55414, United States.ORCID 0000-0003-1755-1485 Gunda I GeorgDepartment of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, College of Pharmacy, University of Minnesota, 717 Delaware Street SE, Minneapolis, Minnesota 55414, United States.ORCID 0000-0002-8900-9460 Funding
No grant is acknowledged in the PubMed record.
6 · The paper itselfAbstract
We report the design and SAR studies of benzopyran-, benzofuran-, and benzothiophene-derived inhibitors of the retinoic acid receptor alpha (RARα) for male contraception. SAR studies identified critical features influencing activity, such as the optimal positioning of antagonism moieties and substituents, leading to the discovery of (
Indexed as
Contraceptive Agents, MaleRetinoic Acid Receptor alphaAdministration, OralAnimalsBiological AvailabilityHumansMaleMiceStructure-Activity RelationshipContraceptive Agents, MaleRetinoic Acid Receptor alpha
Identifiers
PMID42112580
PMCPMC13224095
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