Benzodipyrazoles: a new class of potent CDK2 inhibitors.
Article Details
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D'Alessio R, Bargiotti A, Metz S, Brasca MG, Cameron A, Ermoli A, Marsiglio A, Polucci P, Roletto F, Tibolla M, Vazquez ML, Vulpetti A, Pevarello P
Benzodipyrazoles: a new class of potent CDK2 inhibitors.
Bioorg Med Chem Lett. 2005 Mar 1;15(5):1315-9.
- PubMed ID
- 15713378 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) 1-[4-(AMINOSULFONYL)PHENYL]-1,6-DIHYDROPYRAZOLO[3,4-E]INDAZOLE-3-CARBOXAMIDE Cyclin-dependent kinase 2 IC 50 (nM) 0.3 7.4 22 Details