Benzo[d]imidazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)--Hit to Lead studies

Honghe Wan; Tram Huynh; Suhong Pang; Jieping Geng; Wayne Vaccaro; Michael A Poss; George L Trainor; Matthew V Lorenzi; Marco Gottardis; Lata Jayaraman; Ashok V Purandare

doi:10.1016/j.bmcl.2009.07.040

Benzo[d]imidazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)--Hit to Lead studies

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5063-6. doi: 10.1016/j.bmcl.2009.07.040. Epub 2009 Jul 10.

Authors

Honghe Wan¹, Tram Huynh, Suhong Pang, Jieping Geng, 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, USA. [email protected]

PMID: 19632837
DOI: 10.1016/j.bmcl.2009.07.040

Abstract

Hit to Lead optimization and SAR development led to the identification of the potent and selective benzo[d]imidazole inhibitor (17b) of Co-activator Associated Arginine Methyltransferase (CARM1).

MeSH terms

Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry*
Antineoplastic Agents / pharmacology
Benzimidazoles / chemical synthesis
Benzimidazoles / chemistry*
Benzimidazoles / pharmacology
Drug Design
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology
Piperidines / chemical synthesis
Piperidines / chemistry*
Piperidines / pharmacology
Protein-Arginine N-Methyltransferases / antagonists & inhibitors*
Protein-Arginine N-Methyltransferases / metabolism
Structure-Activity Relationship

Substances

Antineoplastic Agents
Benzimidazoles
Enzyme Inhibitors
Piperidines
Protein-Arginine N-Methyltransferases
coactivator-associated arginine methyltransferase 1