Design, stereoselective synthesis and anticancer efficacy of a new class of functionalized pyrrolizidine heterocyclic hybrids

Eight new functionalized spirooxindole-pyrrolizidine heterocyclic hybrids has been obtained from N-pyr-idinylmethyl-bisarylmethylidene-pyridinones, Isatin and L-Proline by a multi-component cycloaddition reaction. Such synthesized derivatives are being characterized systematically with the aid of instrumental facilities like FT-IR, NMR spectroscopy, and Mass spectrometry. Following this, all the compounds are tested for the anticancer potentials in vitro using HepG2 cells (cancer cells). The compound with no substitution on the aryl rings (phenyl rings), displayed the highest activity among the spirooxindole-pyrrolizidines. Further the most active hetero-cyclic hybrids are verified for toxicity effects against L929 cells (non-cancer cells; at 200 mu g/mL for 24 h). Finally, the cell viability losses for these most active compounds (at its IC50 value) are addressed by assaying the activity of free radicals, apoptosis, and caspases.

Automated summary

Eight new functionalized spirooxindole-pyrrolizidine heterocyclic hybrids have been synthesized and characterized. The compound with no substitution on the aryl rings displayed the highest anticancer activity. The most active compounds were further tested for toxicity effects and their impact on cell viability was investigated by assaying free radicals, apoptosis, and caspases.