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  • Title: N-(indazolyl)benzamido derivatives as CDK1 inhibitors: design, synthesis, biological activity, and molecular docking studies.
    Author: Raffa D, Maggio B, Cascioferro S, Raimondi MV, Daidone G, Plescia S, Schillaci D, Cusimano MG, Titone L, Colomba C, Tolomeo M.
    Journal: Arch Pharm (Weinheim); 2009 May; 342(5):265-73. PubMed ID: 19415659.
    Abstract:
    A series of N-1H-indazole-1-carboxamides has been synthesized and their effects on both CDK1/cyclin B and the K-562 (human chronic myelogenus leukemia) cell line were evaluated. Using a computational model, we have observed that all the most active compounds 9e, f, i-n exhibited the same binding mode of purvanalol A in the ATP-binding cleft. Although they were able to moderately inhibit the leukemic cell line K-562 and to show inhibitory activity against the Cdc2-Cyclin B kinase in the low micromolar range, they turned out to be non-cytotoxic against HuDe (IZSL) primary cell cultures from human derm. These preliminary results are quite encouraging in view of the low toxicity demonstrated by the above-mentioned compounds.
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