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

@article{Asaki2006DesignAS,
  title={Design and synthesis of 3-substituted benzamide derivatives as Bcr-Abl kinase inhibitors.},
  author={Tetsuo Asaki and Yukiteru Sugiyama and Taisuke Hamamoto and Masaya Higashioka and Masato Umehara and Haruna Naito and Tomoko Niwa},
  journal={Bioorganic & medicinal chemistry letters},
  year={2006},
  volume={16 5},
  pages={1421-5}
}
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… CONTINUE READING

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