6-Substituted pyrrolo[3,4-c]pyrazoles: an improved class of CDK2 inhibitors.

  title={6-Substituted pyrrolo[3,4-c]pyrazoles: an improved class of CDK2 inhibitors.},
  author={Maria Gabriella Brasca and Clara Albanese and Raffaella Amici and Dario Ballinari and L. Corti and Valter Croci and Daniele Fancelli and Francesco Fiorentini and Marcella Nesi and Paolo Orsini and Fabrizio Orzi and Wilma Pastori and Ettore Perrone and Enrico Pesenti and Paolo Pevarello and Federico Riccardi-Sirtori and Fulvia Roletto and Patrick Roussel and Mario Varasi and Anna Vulpetti and Ciro Mercurio},
  volume={2 6},
We have recently reported a new class of CDK2/cyclin A inhibitors based on a bicyclic tetrahydropyrrolo[3,4-c]pyrazole scaffold. The introduction of small alkyl or cycloalkyl groups in position 6 of this scaffold allowed variation at the other two diversity points. Conventional and polymer-assisted solution phase chemistry provided a way of generating compounds with improved biochemical and cellular activity. Optimization of the physical properties and pharmacokinetic profile led to a compound… CONTINUE READING