期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 23, 页码 6670-6674出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.10.001
关键词
Kinase; Tie-2; TEK; Inhibition; Angiogenesis; Small molecule
The SAR and improvement in potency against Tie2 of novel thienopyrimidine and thiazolopyrimidine kinase inhibitors are reported. The crystal structure of one of these compounds bound to the Tie-2 kinase domain is consistent with the SAR. These compounds have moderate potency in cellular assays of Tie-2 inhibition, good physical properties, DMPK, and show evidence of in vivo inhibition of Tie-2. (C) 2009 Elsevier Ltd. All rights reserved.
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