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Lonidamine-1,3,4-oxadiazole derivatives with antiproliferative effects on HCT116 colon cancer cell lines: biological
Raveendra Madhukar Bhat1,2, A N Priyadarshini3, M S Sudhanva3
1Centre for Nano and Material Sciences, Jain (Deemed-to-be University) Jain Global Campus, Jakkasandra Post, Kanakapura Road, Ramanagara District Bangalore Karnataka 562112 India sk.rangappa@jainuniversity.ac.in keriphd@gmail.com +918027577199 +919620667075.
Abstract:
In recent years, cancer has emerged as a significant challenge for healthcare systems, posing challenges to researchers to develop new treatments. Among various cancers, colorectal cancer is a major cause of death worldwide. To develop novel compounds that strongly inhibit colon cancer cells, lonidamine-1,3,4-oxadiazole derivatives 7(a-h) were designed and synthesized. The prepared compounds were characterized by various spectral techniques, including NMR (1H and 13C), mass spectra, and HPLC. Cytotoxicity tests conducted on a colorectal cancer cell line indicated that compound (7d) demonstrated significant antiproliferative effects, achieving the lowest IC50 value of 12.91 ± 1.58 µM, thereby making it the most effective among the compounds tested. This compound induces apoptosis, as evidenced by Hoechst/PI double staining, and mitigates cell migration, demonstrating its antiproliferative and antimigratory capabilities. Molecular docking, dynamics simulations, and DFT studies helped clarify the structure-activity relationship (SAR) and mechanisms of action. ADME and toxicity predictions also supported its drug-like properties. SAR analysis identified key substituents influencing activity, guiding further optimization. Overall, compound (7d) appears to be a promising candidate for colon cancer therapy, though additional studies are necessary to assess its clinical potential. These findings could be used for designing novel cancer therapeutic or preventive LND-derived agents.
Insights
Researchers developed novel lonidamine-1,3,4-oxadiazole derivatives to combat colon cancer. Compound (7d) showed significant antiproliferative and antimigratory effects, inducing apoptosis and showing promise for future cancer therapies.
Area of Science:
- Medicinal Chemistry
- Oncology
- Drug Discovery
Background:
- Colorectal cancer remains a leading cause of cancer-related mortality globally.
- Developing effective and novel therapeutic agents for colon cancer is a critical unmet need.
- Lonidamine derivatives are explored for their potential anticancer activities.
Purpose of the Study:
- To design and synthesize novel lonidamine-1,3,4-oxadiazole derivatives.
- To evaluate the antiproliferative and antimigratory potential of these compounds against colorectal cancer cells.
- To elucidate the mechanism of action and structure-activity relationships (SAR) of the most potent compounds.
Main Methods:
- Synthesis of lonidamine-1,3,4-oxadiazole derivatives (7a-h).
- Characterization using NMR, mass spectrometry, and HPLC.
- In vitro cytotoxicity assays (IC50 determination), Hoechst/PI staining for apoptosis, cell migration assays.
- Molecular docking, molecular dynamics simulations, DFT studies, ADME/toxicity predictions.
Main Results:
- Compound (7d) exhibited significant antiproliferative activity with the lowest IC50 value (12.91 ± 1.58 µM).
- Compound (7d) induced apoptosis and reduced cell migration in colorectal cancer cells.
- Computational studies elucidated SAR and mechanism of action, supporting favorable drug-like properties for (7d).
Conclusions:
- Compound (7d), a novel lonidamine-1,3,4-oxadiazole derivative, demonstrates potent anticancer effects against colon cancer cells.
- The findings suggest compound (7d) is a promising candidate for further development in colon cancer therapy.
- This study provides a basis for designing new lonidamine-derived anticancer agents.
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