1. Academic Validation
  2. New pyrazolo[3,4-d]pyrimidines endowed with A431 antiproliferative activity and inhibitory properties of Src phosphorylation

New pyrazolo[3,4-d]pyrimidines endowed with A431 antiproliferative activity and inhibitory properties of Src phosphorylation

  • Bioorg Med Chem Lett. 2004 May 17;14(10):2511-7. doi: 10.1016/j.bmcl.2004.03.013.
S Schenone 1 O Bruno A Ranise F Bondavalli C Brullo P Fossa L Mosti G Menozzi F Carraro A Naldini C Bernini F Manetti M Botta
Affiliations

Affiliation

  • 1 Dipartimento di Scienze Farmaceutiche, Università di Genova, Viale Benedetto XV, I-16132 Genoa, Italy. [email protected]
Abstract

New 4-aminopyrazolo[3,4-d]pyrimidines bearing various substituents at the position 1 and 6, were synthesized. The new compounds showed antiproliferative activity toward A431 cells, were found to be inhibitors of Src phosphorylation, and induced apoptotic cell death. In particular, 2h was a better inhibitor of Src phosphorylation than the reference compound PP2.

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