Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1).
Design, synthesis, and SAR development led to the identification of the potent, novel, and selective pyrazole based inhibitor (7f) of Coactivator Associated Arginine Methyltransferase (CARM1).
Huynh
Tram
T
Bristol-Myers Squibb Pharmaceutical Research and Development, Princeton, NJ 08543, United States.
Chen
Zhong
Z
Pang
Suhong
S
Geng
Jieping
J
Bandiera
Tiziano
T
Bindi
Simona
S
Vianello
Paola
P
Roletto
Fulvia
F
Thieffine
Sandrine
S
Galvani
Arturo
A
Vaccaro
Wayne
W
Poss
Michael A
MA
Trainor
George L
GL
Lorenzi
Matthew V
MV
Gottardis
Marco
M
Jayaraman
Lata
L
Purandare
Ashok V
AV
D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D011484:Protein-Arginine N-Methyltransferases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D011720:Pyrazoles; D011484:Protein-Arginine N-Methyltransferases; C119966:coactivator-associated arginine methyltransferase 1