期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 24, 页码 7653-7658出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.10.007
关键词
JAK1; JAK2; JAK3; 4-Aryl-2-aminoalkylpyrimidine
We report the discovery of a series of 4-aryl-2-aminoalkylpyrimidine derivatives as potent and selective JAK2 inhibitors. High throughput screening of our in-house compound library led to the identification of hit 1, from which optimization resulted in the discovery of highly potent and selective JAK2 inhibitors. Advanced lead 10d demonstrated a significant dose-dependent pharmacodynamic and antitumor effect in a mouse xenograft model. Based upon the desirable profile of 10d (XL019) it was advanced into clinical trials. (C) 2012 Elsevier Ltd. All rights reserved.
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