Author/Authors :
Tao Guo، نويسنده , , Anton E.P. Adang، نويسنده , , Guizhen Dong، نويسنده , , Dan Fitzpatrick، نويسنده , , Peng Geng، نويسنده , , Koc-Kan Ho، نويسنده , , Charles H. Jibilian، نويسنده , , Steven G. Kultgen، نويسنده , , Ruiyan Liu، نويسنده , , B. Edward McDonald and William L. Siegmann، 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 :
Potent small molecule biaryl diketopiperazine FSH receptor agonists such as 10c (EC50=13 nM) and 11f (EC50=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.
Keywords :
FSH Receptor agonists , Parallel synthesis.* Corresponding author. Tel.: +1-609-452-3746 , fax: +1-732-422-0156 , e-mail: tguo@pharmacop.com
