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Cu/Pd catalyzed one pot synthesis of fused benzoxazino[1,2,3]triazolyl[4,5-c]quinolinone hybrids and their cytotoxic activity against human cancer cell lines MCF-7, HeLa and A-549 is described.

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In this report, we describe the synthesis and biological evaluation of a new series of (4‐((1‐(aryl)‐1H‐1,2,3‐triazol‐4‐yl)methoxy)phenyl)(1,1‐dioxidothiomorpholino)methanone derivatives (6 a‐6 n). All the new derivatives were well analyzed by 1H NMR, 13C NMR, FTIR, mass spectral and elemental data. The synthesized compounds were screened for in vitro anticancer activity against three cancer cell lines (MCF‐7, HeLa, and HEK293) and compared with standard drug cisplatin. Three (6 b, 6 g and 6 i) out of fourteen derivatives exhibited potent anticancer activity against MCF‐7, HeLa, and HEK293. Two (6 b and 6 g) potent hybrids were screened for in vivo studies against EAC bearing mice and found to possess potential anticancer activity.