Author/Authors :
Tao Guo، نويسنده , , Anton E.P. Adang، نويسنده , , Roland E. Dolle، نويسنده , , Guizhen Dong، نويسنده , , Dan Fitzpatrick، نويسنده , , Peng Geng، نويسنده , , Koc-Kan Ho، نويسنده , , Steven G. Kultgen، نويسنده , , Ruiyan Liu، نويسنده , , B. Edward McDonald and William L. Siegmann، نويسنده , , Brian F. McGuinness، نويسنده , , Kurt W. Saionz، نويسنده , , Kenneth J. Valenzano، نويسنده , , Nicole C.R. van Straten، نويسنده , , Dan Xie and Guoliang Ji ، نويسنده , , Maria L. Webb، نويسنده ,
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.
Keywords :
Combinatorial synthesis.* Corresponding author. Tel.: +1-609-452-3746 , fax: +1-732-422-0156 , e-mail: tguo@pharmacop.com , Smallmolecule biaryl FSHagonists
