Small molecule biaryl FSH receptor agonists. Part 1
| Autor: | Kenneth J. Valenzano, Kurt W. Saionz, Ruiyan Liu, Dan Xie, Koc-Kan Ho, Edward Mcdonald, Guizhen Dong, Steven G. Kultgen, Peng Geng, Tao Guo, Dan Fitzpatrick, Roland E. Dolle, Anton E.P. Adang, Nicole C.R. van Straten, Brian F. Mcguinness, Maria L. Webb |
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| Rok vydání: | 2004 |
| Předmět: |
Agonist
medicine.drug_class Chemistry Stereochemistry Organic Chemistry Clinical Biochemistry Biphenyl derivatives Pharmaceutical Science Carboxamide Transfection Combinatorial synthesis Biochemistry Combinatorial chemistry Small molecule Drug Discovery medicine Molecular Medicine Follicle-stimulating hormone receptor Molecular Biology |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 14:1713-1716 |
| ISSN: | 0960-894X |
| Popis: | High-throughput screening of two million compounds in 37 distinct encoded combinatorial libraries using FSH receptor transfected cells provided small molecule agonists such as 1 (EC50=3 μM) and 2 (EC50=3.9 μM), based on which a focused combinatorial library with a total of 31,372 compounds was designed, synthesized, and screened to reveal 72 novel biaryl FSH receptor agonists such as 8a–c as well as a unique combinatorial SAR. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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