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
  • 1. Dipartimento di Scienze Farmaceutiche, Università di Genova, Viale Benedetto XV, I-16132 Genoa, Italy. [email protected]
PMID: 15109642 DOI: 10.1016/j.bmcl.2004.03.013
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.