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Synthesis and Biopharmaceutical Evaluation of Imatinib Analogues Featuring Unusual Structural MotifsNicolaou, Kyriacos C; Vourloumis, Dionisios; Totokotsopoulos, Sotirios; Papakyriakou, Athanasios; Karsunky, Holger; Fernando, Hanan; Gavrilyuk, Julia; Webb, Damien; Stepan, Antonia F
ChemMedChem, January 5, 2016, Letnik: 11, Številka: 1Journal Article
A convenient synthesis of imatinib, a potent inhibitor of ABL1 kinase and widely prescribed drug for the treatment of a variety of leukemias, was devised and applied to the construction of a series of novel imatinib analogues featuring a number of non-aromatic structural motifs in place of the parent molecule's phenyl moiety. These analogues were subsequently evaluated for their biopharmaceutical properties (e.g., ABL1 kinase inhibitory activity, cytotoxicity). The bicyclo1.1.1pentane- and cubane-containing analogues were found to possess higher themodynamic solubility, whereas cubane- and cyclohexyl-containing analogues exhibited the highest inhibitory activity against ABL1 kinase and the most potent cytotoxicity values against cancer cell lines K562 and SUP-B15. Molecular modeling was employed to rationalize the weak activity of the compounds against ABL1 kinase, and it is likely that the observed cytotoxicity of these agents arises through off-target effects.
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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