Design, synthesis and biological evaluation of novel pyrazole-based compounds as potential chemotherapeutic agents

Abstract

<b>Aim:</b> Design and synthesis of pyrazole-based chemotherapeutic agents. <b>Materials & methods:</b> A series of novel diphenyl pyrazole-chalcone derivatives were synthesized and assessed for their cytotoxic activities against 14 cancer cell lines and their antimicrobial activities against MRSA and <i>Escherichia coli</i> along with their safety using HSF normal cell line. <b>Results & conclusion:</b> Majority of the compounds showed moderate-to-significant anticancer activity with selective high percentage inhibition (>80%) against HNO-97 while being nontoxic toward normal cells. Compounds <b>6b</b> and <b>6d</b> were the most potent congeners with IC₅₀ of 10 and 10.56 μM respectively. The synthesized compounds exhibited moderate to potent antimicrobial activities. Interestingly, compound <b>6d</b> exhibited a minimum inhibitory concentration of 15.7 μg/ml against MRSA; and a minimum inhibitory concentration of 7.8 μg/ml versus <i>E. coli</i>.