Potent antiproliferative active agents: novel bis Schiff bases and bis spiro β-lactams bearing isatin tethered with butylene and phenylene as spacer and DNA/BSA binding behavior as well as studying molecular docking

cis-Diastereoselective Synthesis of Spirooxindolo-β-Lactams by Staudinger Cycloaddition with TsCl as Activating Co-reagent

“…Since mixed anhydrides of 4-toluene sulfonic acid and carboxylic acids are known to be relatively stable, − the formation of ketene is expected to proceed more slowly, providing a more simple procedure. TsCl is known as an activation co-reagent in β-lactam ring formation reactions. − …”

Synthesis, in-vitro Biological Evaluation, and Molecular Docking Study of Novel spiro-β-lactam-isatin Hybrids

“…1) as well as investigation of their anticancer ability. As a result, several compounds exhibited similar activity to that of cisplatin as positive control [35]. Based on the above mention results, we would like to report the synthesis of some spiro-β-lactam isatin hybrids through Staudinger reaction.…”

“…Well known biologically active compounds like cephalosporin and penicillin have the β-lactam ring in their structure [26]. Among β-lactams, spiro-β-lactams have received special attention since some of their derivatives have exhibited potential pharmaceutical applications including cholesterol absorption inhibition [27], antimalarial [28][29][30][31], antibacterial [32], antiviral [33], anti-HIV [28,29], antioxidant [34], anticancer and antiproliferative [34,35] activities. Moreover, spiro-β-lactams have been also used as synthons for synthesis of heterocycles and other organic compounds [36].…”

Sequential Diimination, Staudinger [2 + 2] Ketene–Imine Cycloaddition, and Ring-Closing Metathesis (RCM) Reactions: In Route to Bis(4-spiro-fused-β-lactams)-Based Macrocycles

“…Deriving novel bis-β-lactams-based unsaturated macrocycles (Figure 1) has received considerable attention with notable impact not only in organic synthesis but also in other research areas such as medicine, pharmaceutical, and supramolecular chemistry. 1 Sequential organic transformations based on (i) formation of diimine substrates, (ii) Staudinger [2 + 2] ketene−imine cycloaddition, and (iii) ring-closing metathesis (Figure 1) have been typically exploited as suitable synthetic procedures for the construction of new bis-2-azetidinone-based azacrown ethers with an unparallel opportunity for researchers to explore their utilities as feasible bioactive materials, owing to the promising biological potentials including antimicrobial, 2,3 antimalarial, 4,5 and anticancer activities 6,7 of the β-lactam site.…”