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Design and synthesis of 3-substituted benzamide derivatives as Bcr-Abl kinase inhibitors.

Abstract：

:A series of 3-substituted benzamide derivatives structurally related to STI-571 (imatinib mesylate), a Bcr-Abl tyrosine kinase inhibitor used to treat chronic myeloid leukemia (CML), was prepared and evaluated for antiproliferative activity against the Bcr-Abl-positive leukemia cell line K562. About ten 3-halogenated and 3-trifluoromethylated benzamide derivatives were identified as highly potent Bcr-Abl kinase inhibitors. One of these, NS-187 (9b), is a promising new candidate Bcr-Abl inhibitor for the therapy of STI-571-resistant chronic myeloid leukemia.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Asaki T,Sugiyama Y,Hamamoto T,Higashioka M,Umehara M,Naito H,Niwa T

doi

10.1016/j.bmcl.2005.11.042

subject

Has Abstract

pub_date

2006-03-01 00:00:00

pages

1421-5

issue

5

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(05)01453-8

journal_volume

16

pub_type

杂志文章

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