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ID: ALA1154366

Journal: Bioorg Med Chem Lett

Title: 1,2-Diamines as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1).

Authors: Therrien E, Larouche G, Manku S, Allan M, Nguyen N, Styhler S, Robert MF, Goulet AC, Besterman JM, Nguyen H, Wahhab A.

Abstract: We have identified the N(1)-benzyl-N(2)-methylethane-1,2-diamine unit as a substitute for the (S)-alanine benzylamide moiety for the design of co-activator associated arginine methyltransferase 1 (CARM1) inhibitors. The potency of these inhibitors is in the same order of magnitude as their predecessors and their clearance, volume of distribution, and half lives were greatly improved.

CiteXplore: 19836951

DOI: 10.1016/j.bmcl.2009.09.110