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Novel series of triazole-benzoxazole hybrid compounds (7a-7i) have been synthesized via click chemistry between different azide derivatives and benzoxazole terminal alkynes bearing an S-methylene linkage. The starting alkyne was prepared via base-catalyzed S-alkylation of benzoxazole substrate in two-step procedures. All the intermediates and the final products were fully characterized by 1D NMR, IR, mass spectrometry, and elemental analysis techniques. The reported hybrids of two heterocyclic rings, i.e., benzoxazole and 1,2,3-triazole in a single structure, were screened for their anticancer activity against nine basic cancer panels as well as NCI-60 cell-line.  In vitro  anticancer studies revealed that the compounds 7b, 7c, 7d, 7i, and 7g showed potent anticancer activity against Leukemia, non-small cell lung cancer, renal cancer, and melanoma cancer cell-lines with GI 50  range from 5.61 to 20.87 µM. The fraction’s anti-microbial activity was found that the targeted scaffolds were not any significant potency in anti-microbial strains.

A Step-By-Step Synthesis of S-Methylene Linker Containing Triazole-Benzoxazole Hybrids by Click Chemistry Approach: Anticancer Activity in Human Cells