Synthesis and in vitro antitumor evaluation of novel Schiff bases

摘要

Abstract Scientific research in the battle against cancer disease leads to the preparation of various antitumor agents with promising results. In this context, a novel series of Schiff bases 11 – 28 derived from 5-amino-1 H -pyrazole-4-carboxamides 4a – c and aromatic aldehydes 5 – 10 is presented together with the synthesize and evaluation for their antitumor activities against HepG2 (liver) and MCF-7 (breast) cell lines using MTT assay. Structure–activity relationship (SAR) is also discussed. The antitumor activities of the Schiff bases 11 – 28 shows that, compound 17 (IC 50 ?=?66.3?±?4.9?μM) is found to be an active candidate against HepG2 cells compared to doxorubicin (IC 50 ?=?80.9?±?2.1?μM) and compound 23 (IC 50 ?=?60.8?±?6.1?μM) is found to be the most potent derivative against MCF-7 than doxorubicin (IC 50 ?=?65.6?±?4.2?μM). Compounds 17 and 23 managed to induce apoptosis in HepG2 and MCF-7, respectively. Both compounds 17 and 23 induced more apoptotic cells and increased in the caspase-3 levels.