• Bioorg. Med. Chem. Lett. · Mar 2005

    Benzodipyrazoles: a new class of potent CDK2 inhibitors.

    • Roberto D'Alessio, Alberto Bargiotti, Suzanne Metz, M Gabriella Brasca, Alexander Cameron, Antonella Ermoli, Aurelio Marsiglio, Paolo Polucci, Fulvia Roletto, Marcellino Tibolla, Michael L Vazquez, Anna Vulpetti, and Paolo Pevarello.
    • Chemistry Department, Nerviano Medical Sciences, Oncology Business Unit, Viale Pasteur 10, 20014 Nerviano (MI), Italy. roberto.dalessio@nervianoms.com
    • Bioorg. Med. Chem. Lett. 2005 Mar 1; 15 (5): 1315-9.

    AbstractThe synthesis and the preliminary expansion of this new class of CDK2 inhibitors are presented. The synthesis was accomplished using a solution-phase protocol amenable to rapid parallel expansion and suitable to be scaled-up in view of possible lead development. Following a medicinal chemistry program aimed at improving cell permeability and selectivity, a series of compounds with nanomolar activity in the biochemical assay and able to efficiently inhibit tumor cell proliferation has been obtained.

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