Pyrazole inhibitors of coactivator associated arginine methyltransferase 1 (CARM1)

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 15, 2008, Pages 4438-4441

  Purandare, Ashok V ^a   Chen, Zhong ^a   Huynh, Tram ^a   Pang, Suhong ^a   Geng, Jieping ^a   Vaccaro, Wayne ^a   Poss, Michael A ^a   Oconnell, Jonathan ^a   Nowak, Kimberly ^a   Jayaraman, Lata ^a  

^a BRISTOL MYERS SQUIBB PHARMACEUTICAL RESEARCH INSTITUTE   (United States)

Author keywords

CARM1; Coactivator associated arginine methyltransferase 1; PRMT4; Protein arginine methyltransferase

Indexed keywords

COACTIVATOR ASSOCIATED ARGININE METHYLTRANSFERASE 1 INHIBITOR; ENZYME INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; DRUG BINDING; DRUG IDENTIFICATION; STRUCTURE ACTIVITY RELATION;

COMBINATORIAL CHEMISTRY TECHNIQUES; MOLECULAR STRUCTURE; PROTEIN-ARGININE N-METHYLTRANSFERASE; PYRAZOLES; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 47849115661     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.06.026     Document Type: Article

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19. a) All compounds were characterized by LC-MS and NMR analysis. In addition, the yields were based on the weight of pure product unless mentioned otherwise. (b) Analytical data for compound 7b: NMR (CD3OD, δ): 8.2 (s, 1H), 7.96 (s, 1H), 7.71 (d, 1H), 7.33 (m, 5H), 7.2 (m, 1H), 7.1 (d, 1H), 4.6 (s, 1H), 4.4 (s, 1H), 3.9 (m, 1H), 1.3 (d, 3H); MS (ESI) m/z 446.18 (M+H).
20. 8 with the following exceptions: GST-PRMT1 or GST-PRMT3, expressed and purified from bacteria, were used as the enzymes instead of CARM1. Histone H4 (Roche Applied Science) was used as the substrate in the PRMT1 assay. GST-GAR, expressed and purified from bacteria, was used as the substrate in the PRMT3 assay.