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Abstract SUMMARY Within the last decades, many researchers had made incredible consideration of the heterocyclic spirooxindole compounds. Numerous changes have been made to overhaul the characteristic movement of the biological activity of natural spirooxindoles and overcome their drawback. In the recent work, we have modified the structure of spirooxindole to increase its activity. Spirooxindoles are exceedingly dynamic heterocyclic arylidene compounds. The stereometric Spirooxindoles were synthesized via the one-pot multi-component 1, 3-dipolar cyclo-addition reaction. This reaction was carried out by reacting up to eight α, β-unsaturated ketones “Chalcones” (3a-h) with isatin and sarcosine in ethanol or methanol under reflux. The reaction progress was monitored by TLC. Final products were purified by column chromatography. from checking on the historical backDROP of oxindole compounds and studying their structure-activity relationships (SARs) relation, we found that the synthesized spirooxindoles have multiple biological activities in numerous targets such as antitumor, antibacterial, and anti-cancer activity. Eight arylidene spirooxindole products (6a-h) showed anti-tumor activity. derivatization of the spirooxindoles including, alkylation, and Mannich Products formations. The next step contains alkylation of 6a and 6b to gives alkyl spirooxindole derivatives (7a, b), (8a, b). The final step includes the Mannich reaction of 6a and 6b to yield (9a-d), (10a, b). All the prepared products were tested for biological evaluation. Molecular docking was performed for all prepared compounds to study their interaction with MDM2 protein as an anti-cancer agent. The prepared spirooxindole derivatives were tested for their biological activity against diverse cancer cell lines. They were tested against B-cell (Lymphoma Cancer), MCF-7 (Breast Cancer Cell Line), MCF-10a (Human Mammary Epithelial Cell Line (Breast Cancer)), and MDA-MB (Breast Cancer Cell Line). One other product we should discuss is chalcone (α, β-unsaturated ketone). Chalcones were intermediates in the preparation of spirooxindoles. They came from a huge category of natural products. There are various methods for the preparation of chalcones in the Literature, but, in our work, we used the Claisen-Schmidt condensation method. This reaction was carried out via the reaction of cyclohexanone with various aryl aldehydes in the presence of an alkaline medium, and at room temperature. Reaction progress was monitored by TLC and final products were crystallized from ethanol to provide immaculate products with high yield. Eight products were synthesized (3a-h) and confirmed with IR and (1H,13C) NMR. Chalcones contains the α, β- unsaturated ketone in their structure, which makes them significantly dynamic compounds. They could be a building blocks for several entities, which makes them good candidates for preparing a colossal class of heterocyclic compounds. The makes them a good candidate for synthesizing spirooxindoles. |