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

S Schenone; O Bruno; A Ranise; F Bondavalli; C Brullo; P Fossa; L Mosti; G Menozzi; F Carraro; A Naldini; C Bernini; F Manetti; M Botta

doi:10.1016/j.bmcl.2004.03.013

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.

Authors

S Schenone¹, O Bruno, A Ranise, F Bondavalli, C Brullo, P Fossa, L Mosti, G Menozzi, F Carraro, A Naldini, C Bernini, F Manetti, M Botta

Affiliation

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / pharmacology
Apoptosis / drug effects
Cell Line, Tumor
Cell Proliferation / drug effects
Dose-Response Relationship, Drug
Humans
Phosphorylation / drug effects
Pyrimidines / chemical synthesis*
Pyrimidines / pharmacology*
Structure-Activity Relationship
src-Family Kinases / antagonists & inhibitors*

Substances

Antineoplastic Agents
Pyrimidines
src-Family Kinases