DESIGN AND SYNTHESIS OF DENSELY FUNCTIONALIZED NOVEL SPIROOXINDOLES AS ANTICANCER AGENTS

P. Shanmugasundaram, D. Easwaramoorthy, Anil Ranu Mhashal, Ayesha Khan

Research output: Contribution to journalArticlepeer-review

Abstract

A series of new Spirooxindole derivatives were designed and synthesized to evaluate their antiproliferative activity by MTT assay. The result revealed most of the compounds exhibited strong antiproliferative properties in comparison with positive control Doxorubicin. Particularly compound 8 showed significant inhibitory activity for both MCF-7 and HeLa cancer cell lines. A molecular docking study was performed to evaluate the potential mechanism of antiproliferative activity. It revealed that designed Spirooxindole derivatives strongly interact with hydrophobic amino acids of the p53 binding site of MDM2. Inhibition of p53-MDM2 interaction results in the reactivation of p53 which is corroborated by the significant antiproliferative activity of the compounds against cancer cell lines. These data signify the potential of designed spirooxindole derivatives as anticancer agents.

Original languageEnglish
Pages (from-to)1599-1604
Number of pages6
JournalRasayan Journal of Chemistry
Volume16
Issue number3
DOIs
StatePublished - 1 Jul 2023
Externally publishedYes

Bibliographical note

Publisher Copyright:
© 2023, Rasayan Journal of Chemistry, c/o Dr. Pratima Sharma. All rights reserved.

Funding

The authors are thankful to the management of the Crescent Institute of Science and Technology for the support of this research work. We are grateful to our colleagues from various departments in the university for the analytical support.

FundersFunder number
Barcelona Institute of Science and Technology

    Keywords

    • 1, 3 Dipolar Cycloaddition
    • Anti-Proliferative Activity
    • Azomethine Ylides
    • Curcumin Analogs
    • Spirooxindole

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