Studies on the synthesis and anticancer activity of diarylpyrazole derivatives

Many researchers are currently working on new therapies that might selectively inhibit the underlying targets for cancer resulting in a better and more complete response with minimal side effects and more improvement on patient?s life quality. Many pyrazole derivatives are well acknowledged to possess a wide range of anticancer bioactivities. The literature survey has revealed that some pyrazole derivatives have been implemented as antileukemic, antitumor and anti-proliferative agents through the inhibition of various enzymes that play important roles in cell division and proliferation. Many compounds owing to different chemical classes as anticancer agents have been developed. Understanding the structural properties of developed compounds is very critical for coherent evaluation of these studies and for developing better molecules. With this encouragement, we have designed diarylpyrazole derivatives bearing quinoline and p-methylphenyl at 1. and 5. positions, respectively. Therefore, we have synthesized a series of piperazine/pyridine amide derivatives starting from 5-(4-methylphenyl)-1-quinoline-2-yl-1H-pyrazole-3-carboxylic acid (Compound 2) and tested their anticancer activities using MTT and sulphorodamine B assays on different cancer cell lines. As a result of MTT assay, we have obtained significant and devolapable cytotoxic activity with BRP51, BRP65 and compounds 3, 4, 6, 8, 10, 12, 13, 14, 15. Among them, compounds 3, 4 and 12 showed the best activitiy on all the cell lines. Calculated IC50 values using the sulforodamine B test resulted that compounds 3, 10 and 12 are the most active ones. Key words: Pyrazole, quinoline, anticancer activity, MTT assay, sulphorodamine B assay