Abstract
AbstractHere we report the synthesis of two‐an acyclic and a macrocyclic‐analogues of thymidine linked to a triazole moiety. The new molecules were synthesized through an intramolecular 1,3‐dipolar cycloaddition reaction of the diazido derivative of thymidine with a suitable alkyne. The acyclic nucleoside showed dose dependent cytotoxicity against glioblastoma and breast cancer cells by causing significant cellular damage as studied with confocal laser scanning microscopy. In silico induced fit molecular docking studies showed poly(ADP‐ribose) polymerase 1 (PARP1) as a potential target of the acyclic nucleoside. On the other hand, both the analogues showed no toxicity against normal fibroblast cells.
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