Microwave-assisted one pot synthesis of fused [1,2,3]triazolo-pyrano[3,2-h]quinolines and their biological evaluation

Abstract

Objectives: Microwave-assisted one-pot synthesis of fused [1,2,3]triazolyl [4',5':4,5]pyrano [3,2-h]quinolines and evaluation of their anticancer activity. Materials and Methods: The newly synthesized compoundswere characterized 1 13by spectroscopic (FTIR, H NMR, C NMR and Mass) analysis after synthesis. All compounds were screened for theirin vitro cytotoxic activity against MCF-7, A-549, and HeLa tumor cell lines using MTT analysis. Results: The results of cytotoxic activity revealedthat compound 3jhas shown potent activity against MCF-7 and HeLa with IC 50 values 16.88 ± 0.5 & 11.42 ± 0.6 μM, which are comparable to the standard drug, doxorubicin. Conclusions: We have developed a new method for the synthesis of fused 1,2 3-triazole derivatives and the protocol involves a Cu-catalyzed one pot [3+2] cycloaddition followed by C-C bond coupling reaction under microwave condition. Most of the analogues showed strong activity against HeLa and moderate activity against MCF-7 and A-549. The results indicate that these compounds have the potential to develop as leads, and their additional simple structural modifications in the title compounds can produce promising anti-cancer agents for the human cervical cancer HeLa cell line.