Synthesis and Structure−Activity Relationship of Novel 6-Aryl-1,4- dihydrobenzo[<i>d</i>][1,3]oxazine-2-thiones as Progesterone Receptor Modulators Leading to the Potent and Selective Nonsteroidal Progesterone Receptor Agonist Tanaproget - Concepedia

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Synthesis and Structure−Activity Relationship of Novel 6-Aryl-1,4- dihydrobenzo[<i>d</i>][1,3]oxazine-2-thiones as Progesterone Receptor Modulators Leading to the Potent and Selective Nonsteroidal Progesterone Receptor Agonist Tanaproget

DOI Full Paper Access

90

Citations

7

References

2005

Year

Andrew Fensome, Reinhold H. W. Bender, Rajiv Chopra, Jeff Cohen, Mark A. Collins, Valerie Hudak, Karl Malakian, Susan Lockhead, Andrea Olland, Kristine Svenson,

Journal of Medicinal Chemistry

Hormonal ContraceptiveOral ContraceptiveReproductive HealthGynecologyOrganic ChemistryPharmacotherapyChemistryPharmaceutical ChemistrySide Effect ProfilesMolecular PharmacologyContraceptionMedicinal ChemistryAdditional SarBiochemistryProgesterone Receptor ModulatorsHormonal ReceptorMechanism Of ActionPharmacological AgentHormonal Male ContraceptionPharmacologyStructure−activity RelationshipCocrystal StructureNatural SciencesMedicineDrug Discovery

Abstract

Tanaproget represents a potential first-in-class nonsteroidal PR agonist for contraception with improved safety and side effect profiles versus currently available steroidal oral contraceptives. Additional SAR, biological activity, and structural information from a tanaproget/hPR-LBD (hPR-LBD = human progesterone receptor ligand binding domain) cocrystal structure will also be presented.

References

	Year	Citations

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