Design and synthesis of 3-substituted benzamide derivatives as Bcr-Abl kinase inhibitors |
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Authors: | Asaki Tetsuo Sugiyama Yukiteru Hamamoto Taisuke Higashioka Masaya Umehara Masato Naito Haruna Niwa Tomoko |
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Institution: | Discovery Research Laboratories, Nippon Shinyaku Co, Ltd, 14 Nishinosho-Monguchi-Cho, Kisshoin, Minami-ku, Kyoto 601-8550, Japan. t.asaki@po.nippon-shinyaku.co.jp |
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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. |
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