Mustafa M Allawi, Ammar A Razzak Mahmood, Lubna H Tahtamouni, Abdulrahman M Saleh, Sana I Kanaan, Khaled M Saleh, Mai F AlSakhen, Nisreen Himsawi, Salem R Yasin
{"title":"作为受体酪氨酸激酶抑制剂的吲哚-6-羧酸酯新衍生物的抗增殖评估。","authors":"Mustafa M Allawi, Ammar A Razzak Mahmood, Lubna H Tahtamouni, Abdulrahman M Saleh, Sana I Kanaan, Khaled M Saleh, Mai F AlSakhen, Nisreen Himsawi, Salem R Yasin","doi":"10.1080/17568919.2024.2347084","DOIUrl":null,"url":null,"abstract":"<p><p><b>Aim:</b> The main goal was to create two new groups of indole derivatives, hydrazine-1-carbothioamide (<b>4a</b> and <b>4b</b>) and oxadiazole (<b>5</b>, and <b>6a-e</b>) that target EGFR (<b>4a</b>, <b>4b</b>, <b>5</b>) or VEGFR-2 (<b>6a-e</b>). <b>Materials & methods:</b> 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 <i>in vitro</i>. <b>Results:</b> Compounds <b>4a</b> (targeting EGFR) and <b>6c</b> (targeting VEGFR-2) were the most effective cytotoxic agents, arresting cancer cells in the G2/M phase and inducing the extrinsic apoptosis pathway. <b>Conclusion:</b> The results of this study show that compounds <b>4a</b> and <b>6c</b> are promising cytotoxic compounds that inhibit the tyrosine kinase activity of EGFR and VEGFR-2, respectively.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":"16 13","pages":"1313-1331"},"PeriodicalIF":3.2000,"publicationDate":"2024-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11318749/pdf/","citationCount":"0","resultStr":"{\"title\":\"Anti-proliferation evaluation of new derivatives of indole-6-carboxylate ester as receptor tyrosine kinase inhibitors.\",\"authors\":\"Mustafa M Allawi, Ammar A Razzak Mahmood, Lubna H Tahtamouni, Abdulrahman M Saleh, Sana I Kanaan, Khaled M Saleh, Mai F AlSakhen, Nisreen Himsawi, Salem R Yasin\",\"doi\":\"10.1080/17568919.2024.2347084\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p><b>Aim:</b> The main goal was to create two new groups of indole derivatives, hydrazine-1-carbothioamide (<b>4a</b> and <b>4b</b>) and oxadiazole (<b>5</b>, and <b>6a-e</b>) that target EGFR (<b>4a</b>, <b>4b</b>, <b>5</b>) or VEGFR-2 (<b>6a-e</b>). <b>Materials & methods:</b> 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 <i>in vitro</i>. <b>Results:</b> Compounds <b>4a</b> (targeting EGFR) and <b>6c</b> (targeting VEGFR-2) were the most effective cytotoxic agents, arresting cancer cells in the G2/M phase and inducing the extrinsic apoptosis pathway. <b>Conclusion:</b> The results of this study show that compounds <b>4a</b> and <b>6c</b> are promising cytotoxic compounds that inhibit the tyrosine kinase activity of EGFR and VEGFR-2, respectively.</p>\",\"PeriodicalId\":12475,\"journal\":{\"name\":\"Future medicinal chemistry\",\"volume\":\"16 13\",\"pages\":\"1313-1331\"},\"PeriodicalIF\":3.2000,\"publicationDate\":\"2024-07-02\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11318749/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Future medicinal chemistry\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1080/17568919.2024.2347084\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/5/10 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Future medicinal chemistry","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/17568919.2024.2347084","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/5/10 0:00:00","PubModel":"Epub","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Anti-proliferation evaluation of new derivatives of indole-6-carboxylate ester as receptor tyrosine kinase inhibitors.
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.
期刊介绍:
Future Medicinal Chemistry offers a forum for the rapid publication of original research and critical reviews of the latest milestones in the field. Strong emphasis is placed on ensuring that the journal stimulates awareness of issues that are anticipated to play an increasingly central role in influencing the future direction of pharmaceutical chemistry. Where relevant, contributions are also actively encouraged on areas as diverse as biotechnology, enzymology, green chemistry, genomics, immunology, materials science, neglected diseases and orphan drugs, pharmacogenomics, proteomics and toxicology.