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Bioorg. Med. Chem. Lett. · Feb 2006
3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors.
- Paolo Pevarello, Daniele Fancelli, Anna Vulpetti, Raffaella Amici, Manuela Villa, Valeria Pittalà, Paola Vianello, Alexander Cameron, Marina Ciomei, Ciro Mercurio, James R Bischoff, Fulvia Roletto, Mario Varasi, and Maria Gabriella Brasca.
- Department of Chemistry, Nerviano Medical Science, BU-Oncology, Via Pasteur 10, 20014 Nerviano MI, Italy. paolo.pevarello@nervianoms.com
- Bioorg. Med. Chem. Lett. 2006 Feb 15; 16 (4): 1084-90.
AbstractWe have recently reported about a new class of Aurora-A inhibitors based on a bicyclic tetrahydropyrrolo[3,4-c]pyrazole scaffold. Here we describe the synthesis and early expansion of CDK2/cyclin A-E inhibitors belonging to the same chemical class. Synthesis of the compounds was accomplished using a solution-phase protocol amenable to rapid parallel expansion. Compounds with nanomolar activity in the biochemical assay and able to efficiently inhibit CDK2-mediated tumor cell proliferation have been obtained.
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