A series of novel morpholines linked coumarin–triazole hybrids (6a–6v) has been synthesized and evaluated for their anti‐proliferative potential on a panel of five human cancer cell lines, namely bone (MG‐63), lung (A549), breast (MDA‐MB‐231), colon (HCT‐15) and liver (HepG2), using MTT assay. Among all, the compound 6n {7‐((1‐(2,4‐dichlorobenzyl)‐1H‐1,2,3‐triazol‐4‐yl) methoxy)‐4‐((2,6‐dimethylmorpholino) methyl)‐2H‐chromen‐2‐one} showed significant growth inhibition against MG‐63 cells with an IC50 value of 0.80 ± 0.22 μM. Further, induction of apoptosis by 6n of MG‐63 cells confirmed as a result of morphological changes, the sub‐G1 phase arrest, increased percentage of apoptotic cells, and decrease in mitochondrial membrane potential and increase in reactive oxygen species levels. The in vitro Gal‐1 expression in cell culture supernatant of MG‐63 cells treated with compound 6n showed dose‐dependent reduction. The binding constant (Ka) of 6n with Gal‐1 was calculated from the intercept value which was observed as 3.0 × 105 M−1 by fluorescence spectroscopy. Surface plasmon resonance showed that 6n binds to Gal‐1 with binding constant (Ka) of 1.29E+04 1/Ms and equilibrium constant KD value of 7.54E−07 M, respectively. Molecular docking studies revealed the binding interactions of 6n with Gal‐1.

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