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Bioorg Med Chem Lett. 2005 Mar 1;15(5):1315-9.

Benzodipyrazoles: a new class of potent CDK2 inhibitors.

Author information

1
Chemistry Department, Nerviano Medical Sciences, Oncology Business Unit, Viale Pasteur 10, 20014 Nerviano (MI), Italy. roberto.dalessio@nervianoms.com

Abstract

The 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.

PMID:
15713378
DOI:
10.1016/j.bmcl.2005.01.023
[Indexed for MEDLINE]

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