Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 23, Pages 6725-6732Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.09.110
Keywords
CARM1 inhibitors; PRMT4 inhibitors; Histone methyltransferase inhibitors; Co-activator associated arginine methyltransferase 1
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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. (C) 2009 Elsevier Ltd. All rights reserved.
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