Aim: The main goal was to create two new groups of indole derivatives, hydrazine-1-carbothioamide (4a and 4b) and oxadiazole (5, and 6a-e) that target EGFR (4a, 4b, 5) or VEGFR-2 (6a-e). Materials & methods: The new derivatives were characterized using various spectroscopic techniques. Docking studies were used to investigate the binding patterns to EGFR/VEGFR-2, and the anti-proliferative properties were tested in vitro. Results: Compounds 4a (targeting EGFR) and 6c (targeting VEGFR-2) were the most effective cytotoxic agents, arresting cancer cells in the G2/M phase and inducing the extrinsic apoptosis pathway. Conclusion: The results of this study show that compounds 4a and 6c are promising cytotoxic compounds that inhibit the tyrosine kinase activity of EGFR and VEGFR-2, respectively.
Anti-proliferation evaluation of new derivatives of indole-6-carboxylate ester as receptor tyrosine kinase inhibitors.
对新型吲哚-6-羧酸酯衍生物作为受体酪氨酸激酶抑制剂的抗增殖活性进行评价
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作者:Allawi Mustafa M, Razzak Mahmood Ammar A, Tahtamouni Lubna H, Saleh Abdulrahman M, Kanaan Sana I, Saleh Khaled M, AlSakhen Mai F, Himsawi Nisreen, Yasin Salem R
| 期刊: | Future Medicinal Chemistry | 影响因子: | 3.400 |
| 时间: | 2024 | 起止号: | 2024 Jul 2; 16(13):1313-1331 |
| doi: | 10.1080/17568919.2024.2347084 | 研究方向: | 其它 |
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