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Vol. 36 No. 11 (2024): Vol 36 Issue 11, 2024

Copyright (c) 2024 P. Shanmugasundaram, D. Easwaramoorthy, J. Herbert Mabel, Srikanth Jeyabalan, Chetan Ashok

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This work is licensed under a Creative Commons Attribution 4.0 International License.

Synthesis, Characterization, in Silico and in vitro Screening of Anticancer Activity of Novel Curcumin Analogues

https://doi.org/10.14233/ajchem.2024.32700
P. Shanmugasundaram
Department of Chemistry, B.S. Abdur Rahman Crescent Institute of Science and Technology, Vandalur-600048, India
https://orcid.org/0009-0003-7403-4895
D. Easwaramoorthy
Department of Chemistry, B.S. Abdur Rahman Crescent Institute of Science and Technology, Vandalur-600048, India
https://orcid.org/0000-0002-3559-0966
J. Herbert Mabel
Department of Chemistry, B.S. Abdur Rahman Crescent Institute of Science and Technology, Vandalur-600048, India
https://orcid.org/0000-0001-7734-7123
Srikanth Jeyabalan
Department of Pharmacology, Sri Ramachandra Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education and Research (DU), Porur, Chennai-600116, India
https://orcid.org/0000-0003-3514-7654
Chetan Ashok
Department of Pharmacology, Sri Ramachandra Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education and Research (DU), Porur, Chennai-600116, India
https://orcid.org/0000-0002-5345-3658

Corresponding Author(s) : P. Shanmugasundaram

pkpshanmugasundaram@gmail.com

Asian Journal of Chemistry, Vol. 36 No. 11 (2024): Vol 36 Issue 11, 2024

Abstract

Global problem of cancer associated side effects with current chemotherapeutics and promising anticancer activity of curcumins, intended present study to carry out the synthesis of some new curcumin analogues using chromone aldehydes and cyclic ketones. The study involved in silico screening and in vitro anticancer evaluation of new synthesized compounds against the breast cancer cell line MDA-MB-231 using the MTT assay. All synthesized compounds exhibited significant cytotoxicity, with IC50 values ranging from 34.04 ± 0.05 µg to 43.96 ± 0.05 µg, comparable to the standard drug cisplatin (IC50 = 29.25 ± 0.14 µg). Among all new synthesized curcumin analogues, compound 2 exhibited the highest anticancer activity. Molecular docking studies supported these findings, demonstrating strong binding affinities of the chromone compounds to key protein targets EGFR (PDB ID: 3UG2) and ERBB2 (PDB ID: 3H3B), critical in breast cancer pathogenesis. The strong cytotoxic effects and binding affinities suggest that curcumin analogues could serve as promising candidates for developing targeted anticancer therapies.

Keywords

Chromone Curcumin analogues Breast cancer Cytotoxicity Molecular docking Targeted therapy
Shanmugasundaram, P., Easwaramoorthy, D., Mabel, J. H., Jeyabalan, S., & Ashok, C. (2024). Synthesis, Characterization, in Silico and in vitro Screening of Anticancer Activity of Novel Curcumin Analogues. Asian Journal of Chemistry, 36(11), 2666–2674. https://doi.org/10.14233/ajchem.2024.32700
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