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Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives.

Abstract：

:To investigate why 3-substituted benzamide derivatives show dual inhibition of Abl and Lyn protein tyrosine kinases, we determined their inhibitory activities against Abl and Lyn, carried out molecular modeling, and conducted a structure-activity relationship study with the aid of a newly determined X-ray structure of the Abl/Lyn dual inhibitor INNO-406 (formerly known as NS-187) bound to human Abl. We found that this series of compounds interacted with both kinases in very similar ways, so that they can inhibit both kinases effectively.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Horio T,Hamasaki T,Inoue T,Wakayama T,Itou S,Naito H,Asaki T,Hayase H,Niwa T

doi

10.1016/j.bmcl.2007.03.002

subject

Has Abstract

pub_date

2007-05-15 00:00:00

pages

2712-7

issue

10

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)00291-0

journal_volume

17

pub_type

杂志文章

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