期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 23, 页码 6725-6732出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.09.110
关键词
CARM1 inhibitors; PRMT4 inhibitors; Histone methyltransferase inhibitors; Co-activator associated arginine methyltransferase 1
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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