期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 27, 期 4, 页码 862-866出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.01.015
关键词
AXL; 7-Azaindole; Receptor tyrosine kinase; Kinase inhibitor; Modeling study; Medicinal chemistry
资金
- ANRT (Agence Nationale de la Recherche et de la Technologie)
AXL is a receptor tyrosine kinase that plays a key role in tumor growth and proliferation. The scientific community has validated AXL as therapeutic target in the treatment of cancers for several years now, and several AXL inhibitors have been developed but none of them are approved. In this context, we started to design new kinase inhibitors targeting AXL from the 7-azaindole scaffold well known to interact with the ATP binding site of the kinase. Focused screening and chemical diversification around 7-azaindole scaffold were developed, based on modeling studies and medicinal chemistry rational, leading to the discovery of a new family of hits with potent inhibitory activity against AXL. (C) 2017 Published by Elsevier Ltd.
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