AI Article Synopsis
- 14 new gefitinib-1,2,3-triazole derivatives were created using click chemistry and analyzed through various methods like H NMR and HRMS.
- Most of these compounds showed strong antitumor activity against lung cancer cells, particularly NCI-H1299, A549, and NCI-H1437.
- Two specific compounds demonstrated significant inhibitory effects and induced cell death by regulating apoptosis-related proteins, suggesting their potential as new lung cancer treatments.
Article Abstract
In this study, 14 structurally novel gefitinib-1,2,3-triazole derivatives were synthesized using a click chemistry approach and characterized by H NMR, C NMR and high-resolution mass spectrometry (HRMS). Preliminary cell counting kit-8 results showed that most of the compounds exhibit excellent antitumor activity against epidermal growth factor receptor wild-type lung cancer cells NCI-H1299, A549 and NCI-H1437. Among them, and showed the most prominent inhibitory effects. The half maximal inhibitory concentration (IC) values of were 4.42 ± 0.24 μM (NCI-H1299), 3.94 ± 0.01 μM (A549) and 1.56 ± 0.06 μM (NCI-1437). The IC values of were 4.60 ± 0.18 µM (NCI-H1299), 4.00 ± 0.08 μM (A549) and 3.51 ± 0.05 μM (NCI-H1437). Furthermore, our results showed that and could effectively inhibit proliferation, colony formation and cell migration in a concentration-dependent manner, as well as induce apoptosis in H1299 cells. In addition, and exerted its anti-tumor effects by inducing cell apoptosis, upregulating the expression of cleaved-caspase 3 and cleaved-PARP and downregulating the protein levels of Bcl-2. Based on these results, it is suggested that and be developed as potential new drugs for lung cancer treatment.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10892142 | PMC |
| http://dx.doi.org/10.3390/molecules29040837 | DOI Listing |
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