SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL PYRAZOLO[3,4-D]PYRIMIDINE DERIVATIVES OF EXPECTED ANTICANCER ACTIVITY

Abstract

A series of novel pyrazolo[3,4-d]pyrimidine derivatives have designed and synthesized in synthetically useful yields. All the new synthesized compounds were biologically evaluated in vitro for their cytotoxic activities against a panel of three cancer cell lines namely, HepG-2, MCF-7, and HCT-116. The results of cytotoxic evaluation indicated that compound (9) exhibited the most prominent cytotoxic effect against all tested cell lines with IC 50 values ranging from (4.03-6.18) µM comparable to that of doxorubicin as a control drug (IC 50 values of 8.17 and 9.27 µM). In particular, compounds (8,9,11) and (12) exhibited higher intercalative activity with IC 50 value of 30 µM than doxorubicin (31 µM).