Journal
FRONTIERS IN CHEMISTRY
Volume 9, Issue -, Pages -Publisher
FRONTIERS MEDIA SA
DOI: 10.3389/fchem.2021.796599
Keywords
schiff base; SEM; anticancer activity; MCF-7; in-silico molecular docking; structure activity relationship
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Funding
- King SaudUniversity, Riyadh, SaudiArabia [RSP-2021/27]
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In this study, chitosan derivatives were synthesized into sulfonated Schiff bases compounds without the use of a catalyst. The synthesized compounds showed high anticancer activity against MCF-7 cancer cells and low cytotoxicity against normal cell lines. In-silico study also revealed that one of the compounds exhibited higher binding affinity for a specific protein, indicating its potential as an anticancer drug.
In this work, we synthesize the sulfonated Schiff bases of the chitosan derivatives 2a-2j without the use of a catalyst in two moderately straightforward steps with good yield within a short reaction time. The morphology and chemical structure of chitosan derivatives were investigated using FT-IR, NMR (H-1-C-13), XRD, and SEM. Furthermore, our chitosan derivatives were tested for their anticancer activity against the MCF-7 cancer cell line, and doxorubicin was used as a standard. In addition, the normal cell lines of the breast cancer cell MCF-10A, and of the lung cell MRC-5 were tested. Compound 2 h, with a GI(50) value of 0.02 mu M for MCF-7, is highly active compared with the standard doxorubicin and other compounds. The synthesized compounds 2a-2j exhibit low cytotoxicity, with IC50 > 100 mu g/ml, against normal cell lines MCF-10A, MRC-5. We also provide the results of an in-silico study involving the Methoxsalen protein (1Z11). Compound 2h exhibits a higher binding affinity for 1Z11 protein (-5.9 kcal/mol) and a lower binding affinity for Doxorubicin (-5.3 kcal/mol) than certain other compounds. As a result of the aforementioned findings, the use of compound 2h has an anticancer drug will be researched in the future.
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