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Identification of potent and selective VEGFR receptor tyrosine kinase inhibitors having new amide isostere headgroups.

Abstract：

:A novel series of malonamide-type dual VEGFR2/c-Met inhibitors in which one of the amide bonds was replaced by an amide isostere-a trifluoroethylamine unit, was designed, synthesized, and evaluated for their enzymatic and cellular inhibition of VEGFR2 and c-Met enzymes. Optimization of these molecular entities resulted in identification of potent and selective inhibitors of VEGFR2 enzyme.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Gaudette F,Raeppel S,Nguyen H,Beaulieu N,Beaulieu C,Dupont I,Macleod AR,Besterman JM,Vaisburg A

doi

10.1016/j.bmcl.2009.12.099

subject

Has Abstract

pub_date

2010-02-01 00:00:00

pages

848-52

issue

3

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)01822-8

journal_volume

20

pub_type

杂志文章

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