Literature DB >> 16580199

Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3.

Raymond J Patch1, Christian A Baumann, Jian Liu, Alan C Gibbs, Heidi Ott, Jennifer Lattanze, Mark R Player.   

Abstract

A series of 2-acylaminothiophene-3-carboxamides has been identified which exhibit potent inhibitory activity against the FLT3 tyrosine kinase. Compound 44 inhibits the isolated enzyme (IC50 = 0.027 microM) and blocks the proliferation of MV4-11 cells (IC50 = 0.41 microM). Structure-activity relationship studies within this series are described in the context of a proposed binding model within the ATP binding site of the enzyme.

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Year:  2006        PMID: 16580199     DOI: 10.1016/j.bmcl.2006.03.032

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  9 in total

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2.  Thiophene derivative-loaded nanoparticles mediate anticancer activity through the inhibition of kinases and microtubule assembly.

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Authors:  Iris Z Uras; Gina J Walter; Ruth Scheicher; Florian Bellutti; Michaela Prchal-Murphy; Anca S Tigan; Peter Valent; Florian H Heidel; Stefan Kubicek; Claudia Scholl; Stefan Fröhling; Veronika Sexl
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Journal:  Mol Pharmacol       Date:  2015-08-05       Impact factor: 4.436

8.  Synthesis, antiproliferative activity and possible mechanism of action of novel 2-acetamidobenzamides bearing the 2-phenoxy functionality.

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Journal:  Bioorg Med Chem       Date:  2015-08-28       Impact factor: 3.641

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  9 in total

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