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ID: ALA1147493

Journal: Bioorg Med Chem Lett

Title: Small molecule biaryl FSH receptor agonists. Part 2: Lead optimization via parallel synthesis.

Authors: Guo T, Adang AE, Dong G, Fitzpatrick D, Geng P, Ho KK, Jibilian CH, Kultgen SG, Liu R, McDonald E, Saionz KW, Valenzano KJ, van Straten NC, Xie D, Webb ML.

Abstract: Potent small molecule biaryl diketopiperazine FSH receptor agonists such as 10c (EC(50)=13 nM) and 11f (EC(50)=1.2 nM) were discovered through the design, synthesis and evaluation of three biaryl diketopiperazine optimization libraries with over 300 compounds. These libraries were prepared via solid-phase parallel synthesis using a cyclization-release method.

CiteXplore: 15026057

DOI: 10.1016/j.bmcl.2004.01.043