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

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• 作者：Tetsuo Asaki ; Yukiteru Sugiyama ; Taisuke Hamamoto ; Masaya Higashioka ; Masato Umehara ; Haruna Naito and Tomoko Niwa
• 关键词：Tyrosine kinase ; Inhibitor ; Bcr-Abl ; Structure– ; activity ; Imatinib
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：1 March 2006
• 年：2006
• 卷：16
• 期：5
• 页码：1421-1425
• 全文大小：201 K

文摘

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.