Small molecule biaryl FSH receptor agonists. Part 2: Lead optimization via parallel synthesis.
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.
Guo
Tao
T
Pharmacopeia, Inc, PO Box 5350, Princeton, NJ 08543-5350, USA. tguo@pharmacop.com
Adang
Anton E P
AE
Dong
Guizhen
G
Fitzpatrick
Dan
D
Geng
Peng
P
Ho
Koc-Kan
KK
Jibilian
Charles H
CH
Kultgen
Steven G
SG
Liu
Ruiyan
R
McDonald
Edward
E
Saionz
Kurt W
KW
Valenzano
Kenneth J
KJ
van Straten
Nicole C R
NC
Xie
Dan
D
Webb
Maria L
ML
D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D010879:Piperazines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D011962:Receptors, FSH / Q000819:agonists* / Q000378:metabolism
D010879:Piperazines; D011962:Receptors, FSH