Design and synthesis of 3-substituted benzamide derivatives as Bcr-Abl kinase inhibitors
Design and synthesis of 3-substituted benzamide derivatives as Bcr-Abl kinase inhibitors
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DOI：
10.1016/j.bmcl.2005.11.042
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发表时间：
2006-03-01
影响因子：
2.7
通讯作者：
Niwa, T
中科院分区：
文献类型：
--
作者：
Asaki, T;Sugiyama, Y;Niwa, T
制备了一系列结构上与STI-571（甲磺酸伊马替尼）（一种用于治疗慢性髓性白血病（CML）的Bcr-Abl酪氨酸激酶抑制剂）相关的3-取代苯甲酰胺衍生物，并评价了其对Bcr-Abl阳性白血病细胞系K562的抗增殖活性。约10个3-卤代和3-三氟甲基苯甲酰胺衍生物被鉴定为高效的Bcr-Abl激酶抑制剂。其中NS-187（9 b）是一种很有前途的Bcr-Abl抑制剂，可用于治疗STI-571耐药的慢性粒细胞白血病。(C)2005爱思唯尔有限公司保留所有权利。
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. (C) 2005 Elsevier Ltd. All rights reserved.