Small molecule biaryl FSH receptor agonists. Part 1: Lead discovery via encoded combinatorial synthesis

Tao Guo, Anton E.P. Adang, Roland E. Dolle, Guizhen Dong, Dan Fitzpatrick, Peng Geng, Koc Kan Ho, Steven G. Kultgen, Ruiyan Liu, Edward McDonald, Brian F. McGuinness, Kurt W. Saionz, Kenneth J. Valenzano, Nicole C.R. Van Straten, Dan Xie, Maria L. Webb

Research output: Contribution to journalArticle

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Abstract

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.

Original languageEnglish
Pages (from-to)1713-1716
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number7
DOIs
StatePublished - Apr 1 2004
Externally publishedYes

Keywords

  • Combinatorial synthesis
  • Small molecule biaryl FSH agonists

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    Guo, T., Adang, A. E. P., Dolle, R. E., Dong, G., Fitzpatrick, D., Geng, P., Ho, K. K., Kultgen, S. G., Liu, R., McDonald, E., McGuinness, B. F., Saionz, K. W., Valenzano, K. J., Van Straten, N. C. R., Xie, D., & Webb, M. L. (2004). Small molecule biaryl FSH receptor agonists. Part 1: Lead discovery via encoded combinatorial synthesis. Bioorganic and Medicinal Chemistry Letters, 14(7), 1713-1716. https://doi.org/10.1016/j.bmcl.2004.01.042