Abstract
New thiourea derivatives bearing a benzodioxole moiety were synthesized via the reaction of 5-isothiocyanatobenzodioxole with amino compounds such as aromatic amines, sulfa drugs, heterocyclic amines, hydrazines and hydrazides. The anticancer activity of the synthesized thiourea derivatives was examined against HCT116, HepG2 and MCF-7 cancer cell lines. Most of thiourea derivatives revealed significant cytotoxic effect, in some cases greater than the doxorubicin. As example, IC50 values of N1,N3-disubstituted-thiosemicarbazone 7 were 1.11, 1.74 and 7.0 μM for HCT116, HepG2 and MCF7, respectively; IC50 values of doxorubicin were 8.29, 7.46 and 4.56 μM, respectively. The anticancer mechanisms were studied via EGFR inhibition and apoptosis assessments, as well as molecular docking.
New series of thiourea derivatives incorporating a benzo[d][1,3]dioxol-5-yl moiety were synthesized and evaluated for anticancer activity. [Display omitted]
•Synthesis of thiourea derivatives incorporating a benzo[d] [1,3]dioxol-5-yl moiety.•Anticancer activity was determined.•EGFR inhibition was determined.•Apoptosis and cell cycle analysis were determined.•Docking study was carried out.