Synthesis, structure–activity relationship, and p210 bcr-abl protein tyrosine kinase activity of novel AG 957 analogs

…, VL Narayanan, PA Risbood, MG Hollingshead…

文献索引：Kaur, Gurmeet; Narayanan, Ven L.; Risbood, Prabhakar A.; Hollingshead, Melinda G.; Stinson, Sherman F.; Varma, Ravi K.; Sausville, Edward A. Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 5 p. 1749 - 1761

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被引用次数: 21

摘要

A series of novel, sterically hindered lipophilic analogs of AG 957 was designed and synthesized as potential protein tyrosine kinase (PTK) inhibitors. The in vitro activity, in vivo anti-leukemia activity, and pharmacology of these PTK inhibitors were studied. Some aspects of the structure–activity relationship associated with the carboxylic acid, phenol ring, and linker modifications are discussed. We have demonstrated that the 1, 4-hydroquinone ...