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Novel Piperidone and Bispidine Derivatives: A New Approach in Cancer Therapy
Cancer remains the second leading cause of death worldwide. As a result, scientists have been trying to find novel therapeutic approaches that target specific metabolic pathways selective to tumor cells. In this study, two novel piperidone and bispidine derivatives, organic molecules that target pol...
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AUC Knowledge Fountain
2025
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| Summary: | Cancer remains the second leading cause of death worldwide. As a result, scientists have been trying to find novel therapeutic approaches that target specific metabolic pathways selective to tumor cells. In this study, two novel piperidone and bispidine derivatives, organic molecules that target polyamine metabolism, were synthesized, and their potential cytotoxic, antioxidant and anti-inflammatory effects were investigated. Polyamines are naturally occurring metabolites that were reported to be in excess at cancer cells and were accounted for tumor proliferation, invasion and metastasis. Accordingly, the novel piperidone and bispidine derivatives were expected to disrupt tumor growth and progression via up-regulation of key enzymes responsible for polyamine catabolism. In vitro studies employing MCF-7, Colo-205, HepG2, and SKOV-3 cell lines were performed. The cell viability of colorectal and ovarian cancer cells in particular was significantly reduced by Bis-1, indicating promising anticancer activity. Additionally, minimal reduction in the cell viability of HSF cell line was reported, suggesting a favorable safety profile against normal healthy cells for both compounds. Another crucial aspect of this research was the assessment of the antioxidant and anti-inflammatory properties of both compounds to investigate if the derivatives have a multifaceted mechanism of action. The results demonstrated that Bis-1 exhibited superior antioxidant effect compared to Bis-2, while the anti-inflammatory effect of Bis-2 was more prominent. Further complexation of the produced derivatives with β-cyclodextrin was performed. The purpose of the complexation was to improve the bioavailability of novel compounds and their transmembrane permeability. Furthermore, it paves the way for future clinical exploration of the cytotoxic, antioxidant and anti-inflammatory effects of the newly synthesized complexes. These findings imply that the novel piperidone and bispidine compounds could be a promising selective cytotoxic agent, overcoming the limitations of current treatments by exerting their anticancer effect with limited damage to healthy tissues. However, further optimization to their chemical structure and bioavailability is still needed. |
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