Facile synthesis of novel substituted aryl-thiazole (SAT) analogs via one-pot multi-component reaction as potent cytotoxic agents against cancer cell lines

In this study, twenty-five (25) substituted aryl thiazoles (SAT) 1-25 were synthesized, and their in vitro cytotoxicity was evaluated against four cancer cell lines, MCF-7 (ER+ve breast), MDA-MB-231 (ER (ve) breast), HCT116 (colorectal) and HeLa (cervical). The activity was compared with the standard anticancer drug doxorubicin (IC50 = 1.56 +/- 0.05 mu M). Among them, compounds 1, 4-8, and 19 were found to be toxic to all four cancer cell lines (IC50 values 5.37 +/- 0.56-46.72 +/- 1.80 mu M). Compound 20 was selectively active against MCF7 breast cancer cells with IC50 of 40.21 +/- 4.15 mu M, whereas compound 19 was active against MCF7 and HeLa cells with IC50 of 46.72 +/- 1.8, and 19.86 +/- 0.11 mu M, respectively. These results suggest that substituted aryl thiazoles 1 and 4 deserve to be further investigated in vivo as anticancer leads. (C) 2016 Elsevier Inc. All rights reserved.