article · Journal of Enzyme Inhibition and Medicinal Chemistry
This research designed and synthesised a new series of 3-phenylthiazolo[3,2-a]benzimidazoles, aiming to create potent anticancer agents that target both tumour cells and cancer stem cells (CSCs). The compounds were evaluated for their anti-proliferative activity against colon cancer (HT-29) and triple-negative breast cancer (MDA-MB-468) cell lines. Their ability to inhibit the cell surface expression of CD133, a CSC marker, was also examined. Compound 4b demonstrated promising anti-proliferative potency against both cell lines and inhibited CD133 expression by 50%, suggesting potential for controlling tumour growth by eradicating tumour bulk and inhibiting CSC proliferation. Compounds 4a and 4c also showed moderate activity.
Cancer stem cells are a major challenge in cancer treatment due to their role in tumour recurrence and resistance. Developing agents that can target both the main tumour cells and these stem cells could lead to more effective therapies, improving patient outcomes and reducing the likelihood of cancer returning.
This early-stage research identifies novel chemical compounds with potential anticancer properties, specifically targeting cancer stem cells and tumour bulk. The identified 'hit molecule' (compound 4b) could serve as a starting point for further drug discovery and development programmes. Future work would involve optimising these compounds and testing them in more complex biological systems, with the ultimate goal of developing new therapeutic agents for cancer patients.
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Cancer stem cells (CSCs) have been objects of intensive study since their identification in 1994. Adopting a structural rigidification approach, a novel series of 3-phenylthiazolo[3,2-a]benzimidazoles 4a-d was designed and synthesised, in an attempt to develop potent anticancer agent that can target the bulk of tumour cells and CSCs. The anti-proliferative activity of the synthesised compounds was evaluated against two cell lines, namely; colon cancer HT-29 and triple negative breast cancer MDA-MB-468 cell lines. Also, their inhibitory activity against the cell surface expression of CD133 was examined. In particular, compound 4b emerged as a promising hit molecule as it manifested good antineoplastic potency against both tested cell lines (IC<sub>50</sub> = 9 and 12 μM, respectively), beside its ability to inhibit the cell surface expression of CD133 by 50% suggesting a promising potential of effectively controlling the tumour by eradicating the tumour bulk and inhibiting the proliferation of the CSCs. Moreover, compounds 4a and 4c showed moderate activity against HT-29 (IC<sub>50</sub> = 21 and 29 μM, respectively) and MDA-MB-468 (IC<sub>50</sub> = 23 and 24 μM, respectively) cell lines, while they inhibited the CD133 expression by 14% and 48%, respectively. Finally, a single crystal X-ray diffraction was recorded for compound 4d.
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DOI: 10.1080/14756366.2017.1347166
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