New pyrazolo[3,4-d]pyrimidines endowed with A431 antiproliferative activity and inhibitory properties of Src phosphorylation.
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.
Schenone
S
S
Dipartimento di Scienze Farmaceutiche, Università di Genova, Viale Benedetto XV, I-16132 Genoa, Italy. schensil@unige.it
Bruno
O
O
Ranise
A
A
Bondavalli
F
F
Brullo
C
C
Fossa
P
P
Mosti
L
L
Menozzi
G
G
Carraro
F
F
Naldini
A
A
Bernini
C
C
Manetti
F
F
Botta
M
M
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D006801:Humans; D010766:Phosphorylation / Q000187:drug effects; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D019061:src-Family Kinases / Q000037:antagonists & inhibitors*
D000970:Antineoplastic Agents; D011743:Pyrimidines; D019061:src-Family Kinases