Synthesis of novel 1H-1,2,3-triazole tethered C-5 substituted uracil–isatin conjugates and their cytotoxic evaluation

The present manuscript describes the synthesis of uracil–isatin hybrids via azide–alkyne cycloadditions and their cytotoxic evaluation against three human cancer cell lines viz. HeLa (cervix), MCF-7 (breast) and DU145 (prostate) using MTT assay. The evaluation studies revealed the dependence of cytotoxicity on C-5 substituents of both uracil and isatin as well as the alkyl chain length with compounds 6g and 6k showing IC50 values 18.21 and 13.90 μM respectively against DU145 cell lines. Most of the synthesized conjugates exhibited considerable selectivity against MCF-7 and DU145 cell lines.

Graphical abstractSynthesis and cytotoxic evaluation of 1H-1,2,3-triazole-tethered uracil–isatin hybrids against a panel of human cancer cell lines have been described.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Synthesis of uracil–isatin hybrids via azide–alkyne cycloaddition reaction. ► Cytotoxic evaluation studies reveal 6g and 6k to be most potent on DU145 cell lines. ► The synthesized conjugates exhibited selectivity against MCF-7 and DU145 cell lines.