학술논문

Novel synthetic aromatic thiourea derivatives and investigations on their cytotoxic potential efficacy.
Document Type
Article
Source
Journal of Heterocyclic Chemistry. Jan2021, Vol. 58 Issue 1, p40-47. 8p.
Subject
*PROPANE
*CARBON disulfide
*CHEMICAL synthesis
*THIOUREA
*CELL lines
*CANCER cells
*ISOTHIOCYANATES
Language
ISSN
0022-152X
Abstract
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. [ABSTRACT FROM AUTHOR]