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).
Bristol-Myers Squibb Pharmaceutical Research and Development, Princeton, NJ 08543, United States.
Tram
T
Huynh
Zhong
Z
Chen
Suhong
S
Pang
Jieping
J
Geng
Tiziano
T
Bandiera
Simona
S
Bindi
Paola
P
Vianello
Fulvia
F
Roletto
Sandrine
S
Thieffine
Arturo
A
Galvani
Wayne
W
Vaccaro
Michael A
MA
Poss
George L
GL
Trainor
Matthew V
MV
Lorenzi
Marco
M
Gottardis
Lata
L
Jayaraman
Ashok V
AV
Purandare
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