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

Salma Mirza, Syeda Asma Naqvi, Khalid Mohammed Khan, Uzma Salar, M Iqbal Choudhary

Bioorganic chemistry 2017 Feb

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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±0.05μM). 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±1.80μM). Compound 20 was selectively active against MCF7 breast cancer cells with IC50 of 40.21±4.15μM, whereas compound 19 was active against MCF7 and HeLa cells with IC50 of 46.72±1.8, and 19.86±0.11μM, respectively. These results suggest that substituted aryl thiazoles 1 and 4 deserve to be further investigated in vivo as anticancer leads. Copyright © 2016 Elsevier Inc. All rights reserved.

Citation

Salma Mirza, Syeda Asma Naqvi, Khalid Mohammed Khan, Uzma Salar, M Iqbal Choudhary. Facile synthesis of novel substituted aryl-thiazole (SAT) analogs via one-pot multi-component reaction as potent cytotoxic agents against cancer cell lines. Bioorganic chemistry. 2017 Feb;70:133-143