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

• DOI: 10.1016/j.ejmech.2011.10.033
• Publication Date: 2011-10-25T20:30:51Z
• Authors: Pardeep Singh; Raghu Raj; Vipan Kumar; Mohinder P. Mahajan; P.M.S. Bedi; Tandeep Kaur; A.K. Saxena
• Keywords: Inhibitory Concentration 50; Chalcone; Cell Line, Tumor; Humans; Antineoplastic Agents; Triazoles; beta-Lactams; 01 natural sciences; Cell Proliferation; 3. Good health; 0104 chemical sciences

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 IC(50) 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.