AI Article Synopsis
- A new series of BIT derivatives were created and tested for their ability to inhibit the growth of specific human cancer cell lines (CaCo-2, HT-29) and a microvascular endothelial cell line (HMVEC-d).
- The most promising compounds (2-4 and 8) were analyzed to understand how they work, showing that they target the microtubule cytoskeleton and cause microtubule accumulation similar to the effects of paclitaxel.
- The findings suggest that these BIT derivatives could be valuable candidates for developing new treatments that target microtubules to combat cancer.
Article Abstract
A series of novel 3,4-dihydrobenzo[4,5]imidazo[1,2-a][1,3,5]triazine (BIT) derivatives were designed and synthesized. In vitro antiproliferative activity was detected toward two human colorectal adenocarcinoma cell lines (CaCo-2 and HT-29) and one human dermal microvascular endothelial cell line (HMVEC-d). The most active compounds, namely 2-4 and 8, were further investigated to clarify the mechanism behind their biological activity. Through immunofluorescence assay, we identified the target of these molecules to be the microtubule cytoskeleton with subsequent formation of dense microtubule accumulation, particularly at the periphery of the cancer cells, as observed in paclitaxel-treated cells. Overall, these results highlight BIT derivatives as robust and feasible candidates deserving to be further developed in the search for novel potent antiproliferative microtubule-targeting agents.
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| http://dx.doi.org/10.1002/ardp.202200295 | DOI Listing |
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