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, Maria Gabriella Brasca

Research output: Contribution to journalArticlepeer-review

Abstract

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.

Original languageEnglish
Pages (from-to)1084-1090
Number of pages7
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number4
DOIs
Publication statusPublished - Feb 15 2006

Keywords

  • CDK2
  • Cyclins
  • Kinase selectivity
  • Tumor cell proliferation inhibition

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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