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Bioorg Med Chem Lett. 2012 Dec 15;22(24):7634-40. doi: 10.1016/j.bmcl.2012.10.016. Epub 2012 Oct 11.

Modification of a promiscuous inhibitor shifts the inhibition from γ-secretase to FLT-3.

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1
Clemens Schöpf-Institute of Organic Chemistry and Biochemistry, Technische Universität Darmstadt, Petersenstr. 22, D-64287 Darmstadt, Germany.

Abstract

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/γ-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 γ-secretase activity and enhanced FLT-3 inhibition.

PMID:
23107479
DOI:
10.1016/j.bmcl.2012.10.016
[Indexed for MEDLINE]
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