In this research, a new series of ( E) -3-(4-substitutedphenyl)-1-(4'-morpholinophenyl)prop-2-en-1-one derivatives 1-7 was synthesized, aiming to develop effective antiproliferative agents. The antiproliferative activities of compounds 1-7 were examined against HeLa and C6 cell lines at eight different concentrations using the BrdU ELISA assay.The activity results were compared with reference anticancer drug 5-fluorouracil (5-FU). Compound 1 had almost the same antiproliferative activity as 5-FU. Compounds 1-7 were found to have greater effects against the C6 cell line than the HeLa cell line. These compounds were also tested in order to determine their effects on enzyme activities. Compounds 2 and 3 exhibited strong activator characteristics against pyruvate kinase isoenzyme M2 (PKM2) with AC 50 values of 2.2 and 14.28 µ M. Compounds 2, 3, and 7 acted as inhibitors with IC 50 values in the range of 84.08-165.38 µ M for carbonic anhydrase isoenzyme I (hCA I), and compounds 3 and 4 demonstrated inhibitory effects against carbonic anhydrase isoenzyme II (hCA II) with IC 50 values of 108.11 and 112.52 µ M, respectively. hCA II was activated by derivatives 1, 2, 6, and 7 with AC 50 values in the range of 85.53-146.59 µ M.
A series of E-4-(3-oxo-3-(substituted)prop-1-en-1-yl)benzoic acid derivatives (1-5) were synthesized by the Claisen-Schmidt condensation of various ketones with 4-formylbenzoic acid. The anticholinesterase (AChE and BChE), tyrosinase, and urease inhibition activities of the synthesized compounds (1-5) were examined. It was found that the most active compound against AChE enzyme in anticholinesterase inhibition activity was compound 1. Compound 4 was the most active compound in tyrosinase inhibition activity, while compound 3 was the most active compound in urease psychological activity.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.