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  • Novel Microtubule-Targeting 7-Deazahypoxanthines Derived from Marine Alkaloid Rigidins with Potent in Vitro and in Vivo Anticancer Activities JOURNAL OF MEDICINAL CHEMISTRY Medellin, D. C., Zhou, Q., Scott, R., Hill, R., Frail, S. K., Dasari, R., Ontiveros, S. J., Pelly, S. C., van Otterlo, W. L., Betancourt, T., Shuster, C. B., Hamel, E., Bai, R., LaBarbera, D. V., Rogelj, S., Frolova, L. V., Kornienko, A. 2016; 59 (1): 480–85


    Docking studies of tubulin-targeting C2-substituted 7-deazahypoxanthine analogues of marine alkaloid rigidins led to the design and synthesis of compounds containing linear C2-substituents. The C2-alkynyl analogue was found to have double- to single-digit nanomolar antiproliferative IC50 values and showed statistically significant tumor size reduction in a colon cancer mouse model at nontoxic concentrations. These results provide impetus and further guidance for the development of these rigidin analogues as anticancer agents.

    View details for DOI 10.1021/acs.jmedchem.5b01426

    View details for Web of Science ID 000368564400034

    View details for PubMedID 26641132

    View details for PubMedCentralID PMC4950951