AI Article Synopsis
- A new strategy in chemotherapy involves creating dual-acting molecules that combine two effective chemo-active groups, which may improve treatment results and reduce side effects when compared to traditional single-target drugs.
- The researchers focused on synthesizing and testing dual-acting levofloxacin-HDACi conjugates that can inhibit both histone deacetylase (HDAC) and tubulin polymerization, showing strong efficacy against HDACs.
- The study found that these conjugates were especially effective against MCF-7 cancer cells, displaying powerful anticancer properties without harming normal cells or causing toxicity.
Article Abstract
A strategy to develop chemotherapy agents by combining two complimentary chemo-active groups into a single molecule may have higher efficacy and fewer side effects than that of single-target drugs. In this article, we describe the synthesis and evaluation of a series of novel dual-acting levofloxacin-HDACi conjugates to target both histone deacetylase (HDAC) and tubulin polymerization. These bifunctional conjugates exhibited potent inhibitory activities against HDACs and tubulin polymerization. In docking analysis provides a structural basis for HDACs inhibition activities. Moreover, these conjugates showed selective anticancer activity that is more potent against MCF-7 compared to other four cancer cells A549, HepG2, PC-3, HeLa, but they had no toxicity toward normal cells.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9080233 | PMC |
| http://dx.doi.org/10.1039/c8ra02578a | DOI Listing |
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