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Bioorg Med Chem Lett. 2006 Mar 1;16(5):1421-5. Epub 2005 Dec 5.

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

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  • 1Discovery Research Laboratories, Nippon Shinyaku Co, Ltd, 14 Nishinosho-Monguchi-Cho, Kisshoin, Minami-ku, Kyoto 601-8550, Japan.


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.

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