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A novel combinatorial library of ester and amide derivatives of 1,3-diarylpyrazoles was designed and synthesized. Anticancer activities of these compounds were assessed against MCF7, MDA-MB-231, HeLa, Raji, and HL60 human cancer cells by MTT assay. Out of these, compounds
4c
and
5f
were found as the most promising anticancer agents with IC
50
values of 8.12 and 9.63 μM in Raji cells, respectively. All compounds exhibited suitable drug-like characteristics according to Lipinski’s rule.