Abstrakt

Synthesis and antitumor activity of novel pyrazolo [3,4-d]pyrimidin-4(5H)-one derivatives

Manal M.Kandeel, Sameha M.Ali, Eman K.A.Abed El All, Mohamed A.Abdelgawad, Phoebe F.Lamie

Starting from pyrazolo[3,4-d]pyrimidine ethyl ester 4 and its corresponding acid hydrazide 5, several new compounds were synthesized such as schiff bases 6a-e, acetyl azide derivative 7, phthalimido derivatives 8, compounds containing oxadiazole ring 9,10a-c, triazole ring system11, 14,15, thiadiazole moiety 13 and phenyl thiosemicarbazide part 12. Some of the synthesized compounds were screened for their antitumor activity against human breast adenocarcinoma cell line (MCF-7) using doxorubicin as a positive control. Compounds 6d, 10b, 12 were found to exhibit good cytotoxic activitywith IC50 equal to (4.6, 4.6, 4.8 ìg/mL), respectively.