Novel synthetic aromatic thiourea derivatives and investigations on their cytotoxic potential efficacy

Aromatic thiourea derivatives were synthesized by standard reactions from isothiocyanates in high yield. An efficient one-pot synthesis of primary amine with carbon disulfide involving the intermediate dithiocarbamate conversion using T₃P (propane phosphonic anhydride) to isothiocyanate is reported. Newly synthesized compounds showed excellent luminescence property. Cytotoxic investigation with different human cancer cell lines showed IC₅₀ values varying from of 17 to 40 μM for N-phenethyl-3,4-dihydroisoquinoline-2(1H)-carbothioamide (SCR172) among other molecules. Increase in Sub G1 population and increased depolarisation of mitochondria were evident in cells treated with SCR172, suggesting its role as a cancer therapeutic agent. This provides a lead structure for further synthetic modifications.