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

E Therrien, G Larouche, S Manku, M Allan…

Index: Therrien, Eric; Larouche, Guillaume; Manku, Sukhdev; Allan, Martin; Nguyen, Natalie; Styhler, Sylvia; Robert, Marie-France; Goulet, Anne-Christine; Besterman, Jeffrey M.; Nguyen, Hannah; Wahhab, Amal Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 23 p. 6725 - 6732

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Citation Number: 37

Abstract

We have identified the N1-benzyl-N2-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.