article · Journal of Enzyme Inhibition and Medicinal Chemistry
Researchers have designed and synthesised a new series of chemical molecules known as benzofuran-isatin conjugates to evaluate their potential against cancer. Several of these compounds were tested across fifty-five human cancer cell lines, where a variant termed 5d demonstrated broad activity across nearly all subpanels. When tested against the SW-620 and HT-29 colorectal cancer cell lines, all synthesised conjugates showed anti-proliferative capabilities. Compounds 5a and 5d showed the strongest inhibitory effects alongside selective cytotoxicity and a good safety profile. Further investigation into their cellular effects revealed that both compounds induced programmed cell death, or apoptosis, in SW-620 cells in a dose-dependent manner. This mechanism operated by decreasing the expression of the anti-apoptotic Bcl2 protein and raising the levels of cleaved PARP.
Colorectal cancer remains a widespread disease that demands targeted and less toxic therapeutic options. Finding compounds that kill tumour cells without causing undue harm to healthy tissue is a key objective in oncology. By demonstrating strong growth inhibition and activating natural cell death pathways in colon cancer cells, these molecules provide useful starting points for developing future cancer treatments.
This research could support the development of novel small-molecule drugs for oncology, particularly for colorectal cancer. The most likely users of these findings are pharmaceutical firms and drug discovery teams looking for candidate molecules. The technology is at an early research stage, having been verified solely in cell-line models, and will require extensive preclinical validation, animal testing, and safety studies before any commercial clinical pipeline can be pursued.
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In the current work, a new set of carbohydrazide linked benzofuran-isatin conjugates (<b>5a-e</b> and <b>7a-i</b>) was designed and synthesised. The anticancer activity for compounds (<b>5b-d</b>, <b>7a, 7b, 7d</b> and <b>7g</b>) was measured against NCI-55 human cancer cell lines. Compound <b>5d</b> was the most efficient, and thus subjected to the five-dose screen where it showed excellent broad activity against almost all tested cancer subpanels. Furthermore, all conjugates (<b>5a-e</b> and <b>7a-i</b>) showed a good anti-proliferative activity towards colorectal cancer SW-620 and HT-29 cell lines, with an excellent inhibitory effect for compounds <b>5a</b> and <b>5d</b> (IC<sub>50</sub> = 8.7 and 9.4 µM (<b>5a</b>), and 6.5 and 9.8 µM for (<b>5d</b>), respectively). Both compounds displayed selective cytotoxicity with good safety profile. In addition, both compounds provoked apoptosis in a dose dependent manner in SW-620 cells. Also, they significantly inhibited the anti-apoptotic Bcl2 protein expression and increased the cleaved PARP level that resulted in SW-620 cells apoptosis.
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DOI: 10.1080/14756366.2021.1944127
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