AI Article Synopsis
- * One specific derivative showed strong cytotoxic effects at low concentrations in two different NSCLC cell lines, while exhibiting less toxicity toward healthy fibroblasts.
- * The mechanism of action for the effective derivative involved inducing apoptosis and halting the cell cycle at the G2/M phase, suggesting potential for future development as targeted cancer therapeutics.
Article Abstract
Five heterocyclic derivatives were synthesized by functionalization of a flavone nucleus with an aminophenoxy moiety. Their cytotoxicity was investigated in vitro in two models of human non-small cell lung cancer (NSCLC) cells (A549 and NCI-H1975) by using MTT assay and the results compared to those obtained in healthy fibroblasts as a non-malignant cell model. One of the aminophenoxy flavone derivatives () was found to be effective at low micromolar concentrations in both lung cancer cell lines with a higher selective index (SI). Flow cytometric analyses showed that induced apoptosis and cell cycle arrest in the G2/M phase through the up-regulation of p21 expression. Therefore, the aminophenoxy flavone-based compounds may be promising cancer-selective agents and could serve as a base for further research into the design of flavone-based anticancer drugs.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10096842 | PMC |
| http://dx.doi.org/10.3390/molecules28073239 | DOI Listing |
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