Synthesis, Anti-Cancer Screening and Molecular Docking of Saccharine-Triazole Hybrid Molecules using Copper(I) Catalyzed Click Chemistry

Abstract

Herein, we report the synthesis methodology and anticancer evaluation of 15 compounds using copper(I)- catalyzed azide alkyne cycloaddition (CuAAC) to develop a library of saccharin-1,2,3-triazole hybrid molecules. All library compounds showed interactions with various amino acids via the basic sulphonamide and amide linkage of the parental saccharin core motif. Molecular docking studies indicated that alternative positions of saccharin-1,2,3-triazole hybrid molecules added a diversity to the potential hydrogen bonding interactions of these compounds with various amino acids. Present results revealed that hybrid derivatives of saccharin which was prepared from saccharin azide was high yield using CuAAC approach. The compounds showed a moderate anti-cancer activity against SK-OV-3 ovarian cancer cell line and could be considered for the development of potential anticancer drugs based on these new molecules.