Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)

Tram Huynh; Zhong Chen; Suhong Pang; Jieping Geng; Tiziano Bandiera; Simona Bindi; Paola Vianello; Fulvia Roletto; Sandrine Thieffine; Arturo Galvani; Wayne Vaccaro; Michael A Poss; George L Trainor; Matthew V Lorenzi; Marco Gottardis; Lata Jayaraman; Ashok V Purandare

doi:10.1016/j.bmcl.2009.04.075

Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)

Bioorg Med Chem Lett. 2009 Jun 1;19(11):2924-7. doi: 10.1016/j.bmcl.2009.04.075. Epub 2009 Apr 22.

Authors

Tram Huynh¹, Zhong Chen, Suhong Pang, Jieping Geng, Tiziano Bandiera, Simona Bindi, Paola Vianello, Fulvia Roletto, Sandrine Thieffine, Arturo Galvani, Wayne Vaccaro, Michael A Poss, George L Trainor, Matthew V Lorenzi, Marco Gottardis, Lata Jayaraman, Ashok V Purandare

Affiliation

¹ Bristol-Myers Squibb Pharmaceutical Research and Development, Princeton, NJ 08543, United States.

PMID: 19419866
DOI: 10.1016/j.bmcl.2009.04.075

Abstract

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).

MeSH terms

Drug Design
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology
Humans
Protein-Arginine N-Methyltransferases / antagonists & inhibitors*
Protein-Arginine N-Methyltransferases / metabolism
Pyrazoles / chemical synthesis
Pyrazoles / chemistry*
Pyrazoles / pharmacology
Structure-Activity Relationship

Substances

Enzyme Inhibitors
Pyrazoles
Protein-Arginine N-Methyltransferases
coactivator-associated arginine methyltransferase 1