Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 24, Pages 7634-7640Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.10.016
Keywords
Acute myeloid leukemia; FLT-3; Kinase inhibitor; gamma-Secretase
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The inhibition of FLT-3 activity is an interesting target for the treatment of acute myeloid leukemia (AML). The serendipitous identification of FLT-3 inhibitors from a CK1/gamma-secretase programme provided compounds with dual inhibitory activity. We analyzed the structure-activity relationship of these inhibitors and derivatized them to arrive at compounds with reduced impact on gamma-secretase activity and enhanced FLT-3 inhibition. (C) 2012 Elsevier Ltd. All rights reserved.
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