Pyrazolo[3,4-d]pyrimidines endowed with antiproliferative activity on ductal infiltrating carcinoma cells.
Novel 1,4,6-trisubstituted pyrazolo[3,4-d]pyrimidines are reported with preliminary in vitro activity data indicating that several of them are potent inhibitors (better than the reference compound) of Src phosphorylation of the breast cancer cells 8701-BC, known to overexpress Src. The ability of such compounds to significantly reduce 8701-BC cell proliferation suggests that this scaffold could be a promising lead for the development of antitumoral agents able to block Src phosphorylation of breast cancer cells.
Carraro
Fabio
F
Dipartimento di Fisiologia, Unità di Fisiologia Cellulare e Molecolare, Università degli Studi di Siena, Via Aldo Moro, I-53100 Siena, Italy.
Pucci
Annalisa
A
Naldini
Antonella
A
Schenone
Silvia
S
Bruno
Olga
O
Ranise
Angelo
A
Bondavalli
Francesco
F
Brullo
Chiara
C
Fossa
Paola
P
Menozzi
Giulia
G
Mosti
Luisa
L
Manetti
Fabrizio
F
Botta
Maurizio
M
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001943:Breast Neoplasms; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D015151:Immunoblotting; D010766:Phosphorylation; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D019061:src-Family Kinases / Q000378:metabolism
D000970:Antineoplastic Agents; D011720:Pyrazoles; D011743:Pyrimidines; D019061:src-Family Kinases