New chroman-4-one/thiochroman-4-one derivatives as potential anticancer agents

Saudi Pharm J. 2017 Nov;25(7):1063-1072. doi: 10.1016/j.jsps.2017.04.040. Epub 2017 Apr 26.

Abstract

The synthesis of 3-[3/4-(2-aryl-2-oxoethoxy)arylidene]chroman/thiochroman-4-one derivatives (1-34) and evaluation of their anticancer activities were aimed in this work. Final compounds were obtained in multistep synthesis reactions using phenol/thiophenol derivatives as starting materials. For anticancer activity evaluation, all compounds were offered to National Cancer Institute (NCI), USA and selected ones were tested against sixty human tumor cell lines derived from nine neoplastic diseases. The activity results were evaluated according to the drug screening protocol of the institute. Compounds containing thiochromanone skeleton exhibited higher anticancer activity.

Keywords: Anticancer activity; Benzopyranone; Benzothiopyranone; Chromanone; Flavone; Thiochromanone; α,β-Unsaturated carbonyl.