We 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. © 2005 Elsevier Ltd. All rights reserved.
CITATION STYLE
Pevarello, P., Fancelli, D., Vulpetti, A., Amici, R., Villa, M., Pittalà, V., … Brasca, M. G. (2006). 3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: A new class of CDK2 inhibitors. Bioorganic and Medicinal Chemistry Letters, 16(4), 1084–1090. https://doi.org/10.1016/j.bmcl.2005.10.071
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