article · Journal of Enzyme Inhibition and Medicinal Chemistry
Researchers synthesised novel series of coumarin-6-sulfonamide derivatives and evaluated their ability to inhibit the growth of three human cancer cell lines in laboratory tests: HepG2 liver cancer, MCF-7 breast cancer, and Caco-2 colon cancer. The liver cancer cells proved the most sensitive to these chemical agents. Among the synthesised variants, compounds 13a and 15a exhibited the strongest anti-proliferative activity against HepG2 cells. Both compounds promoted programmed cell death, or apoptosis, evidenced by the upregulation of Bax, downregulation of Bcl-2, and increased levels of caspase-3. Compound 13a also caused substantial cell cycle arrest at the G2-M phase and noticeably increased the percentage of apoptotic cells. Additionally, quantitative structure-activity relationship models were established to clarify the specific chemical features governing these anti-cancer effects.
Developing effective cancer therapies relies on discovering new molecules that selectively stop tumour cells from multiplying and trigger their natural self-destruction pathways. Demonstrating how specific chemical modifications successfully halt liver cancer cell growth in laboratory cultures, combined with predictive models that map effective molecular structures, provides a foundation for designing more targeted candidate compounds for cancer research.
This work represents early-stage drug discovery that could interest pharmaceutical companies and medicinal chemistry teams seeking lead structures for liver cancer therapeutics. The identified compounds and predictive structural models offer starting points for chemical optimisation. However, because the findings are limited entirely to in vitro cell cultures, the research remains at a fundamental laboratory stage and is far from preclinical or clinical application.
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Herein, we report the synthesis of different novel sets of coumarin-6-sulfonamide derivatives bearing different functionalities (4a, b, 8a-d, 11a-d, 13a, b, and 15a-c), and in vitro evaluation of their growth inhibitory activity towards the proliferation of three cancer cell lines; HepG2 (hepatocellular carcinoma), MCF-7 (breast cancer), and Caco-2 (colon cancer). HepG2 cells were the most sensitive cells to the influence of the target coumarins. Compounds 13a and 15a emerged as the most active members against HepG2 cells (IC<sub>50</sub> = 3.48 ± 0.28 and 5.03 ± 0.39 µM, respectively). Compounds 13a and 15a were able to induce apoptosis in HepG2 cells, as assured by the upregulation of the Bax and downregulation of the Bcl-2, besides boosting caspase-3 levels. Besides, compound 13a induced a significant increase in the percentage of cells at Pre-G1 by 6.4-folds, with concurrent significant arrest in the G2-M phase by 5.4-folds compared to control. Also, 13a displayed significant increase in the percentage of annexin V-FITC positive apoptotic cells from 1.75-13.76%. Moreover, QSAR models were established to explore the structural requirements controlling the anti-proliferative activities.
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DOI: 10.1080/14756366.2018.1477137
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