title: 1,2,3-Triazole tethered β-lactam-chalcone bifunctional hybrids: synthesis and anticancer evaluation.
abstract: 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.
authors.affiliation: Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.
authors.forename: Pardeep
authors.initials: P
authors.lastname: Singh
authors.forename: Raghu
authors.initials: R
authors.lastname: Raj
authors.forename: Vipan
authors.initials: V
authors.lastname: Kumar
authors.forename: Mohinder P
authors.initials: MP
authors.lastname: Mahajan
authors.forename: P M S
authors.initials: PM
authors.lastname: Bedi
authors.forename: Tandeep
authors.initials: T
authors.lastname: Kaur
authors.forename: A K
authors.initials: AK
authors.lastname: Saxena
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002599:Chalcone / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D014230:Triazoles / Q000737:chemistry*; D047090:beta-Lactams / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D014230:Triazoles; D047090:beta-Lactams; D002599:Chalcone