1,2,3-Triazole tethered β-lactam-Chalcone bifunctional hybrids: Synthesis and anticancer evaluation

The manuscript describes the synthesis of novel 1,2,3-triazole tethered β-lactam-chalcone bifunctional hybrids via click chemistry approach utilizing azide-alkyne cycloaddition reactions and their evaluation as anticancer agents against four human cancer cell lines. The presence of a cyclohexyl substituent at N-1 of β-lactam ring and methoxy substituents, preferably ortho on ring A and para on ring B on chalcones markedly improved the anticancer profiles of the synthesized scaffolds with the most potent of the test compound exhibiting an IC50 value of <1, 67.1, <1 and 6.37 μM against A-549(lung), PC-3(prostate), THP-1(leukemia), and Caco-2(colon) cell lines, respectively.

A series of -lactam-chalcone bifunctional hybrids were synthesized and screened for their anti-cancer evaluation.Figure optionsDownload as PowerPoint slideHighlights
► Synthesis and anticancer screening of a series of -lactam-chalcone hybrids.
► Cyclohexyl and methoxy groups improved the anticancer profiles.
► The active compound 6a exhibited an IC50 value of <1, 67.1, <1 and 6.37 μM.