کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1367525 | 981635 | 2006 | 5 صفحه PDF | دانلود رایگان |
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.
A series of 3-substituted benzamide derivatives of STI-571 (imatinib mesylate) was prepared and evaluated for antiproliferative activity against the Bcr-Abl-positive leukemia cell line K562. Several 3-halogenated and 3-trifluoromethylated compounds, including NS-187, showed excellent potency.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 5, 1 March 2006, Pages 1421–1425