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

…, Y Sugiyama, T Hamamoto, M Higashioka…

Index: Asaki, Tetsuo; Sugiyama, Yukiteru; Hamamoto, Taisuke; Higashioka, Masaya; Umehara, Masato; Naito, Haruna; Niwa, Tomoko Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 5 p. 1421 - 1425

Full Text: HTML

Citation Number: 52

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- ...