{"title":"用于治疗肝细胞癌的新型索拉非尼类似物的合成、表征和抗增殖评价。","authors":"Marwan Imad Jihad, Monther Faisal Mahdi","doi":"10.4103/JAPTR.JAPTR_282_23","DOIUrl":null,"url":null,"abstract":"<p><p>Cancer is a disease triggered by an uncontrolled proliferation of a cluster of cells, typically originating from a single cell. Sorafenib, a widely utilized pharmaceutical, has limitations in clinical use due to pharmacokinetic challenges and the development of resistance mechanisms. This investigation aimed to synthesize new sorafenib analogs and evaluated their activity against HepG2 cell lines, specifically targeting hepatocellular carcinoma (HCC). Seven sorafenib analogs were synthesized and identified by Fourier-transform infrared spectroscopy and 1H-NMR spectra. Cytotoxicity of the analogs was assessed on the human HepG2 cancer cell line by (3-(4, 5-dimethylthazolk-2-yl)-2, 5-diphenyl tetrazolium bromide) colorimetric assay. Results revealed that among the studied compounds, 4b exhibited the most pronounced cytotoxicity against cancer cells, surpassing even the efficacy of sorafenib. This suggested that small substitutions on the NH moiety play a crucial role in the activity against the human HepG2 liver cancer cell line. These findings provide valuable insights for the development of potential anticancer-targeting HCC.</p>","PeriodicalId":14877,"journal":{"name":"Journal of Advanced Pharmaceutical Technology & Research","volume":"14 3","pages":"274-279"},"PeriodicalIF":1.4000,"publicationDate":"2023-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/e4/c3/JAPTR-14-274.PMC10483918.pdf","citationCount":"0","resultStr":"{\"title\":\"Synthesis, characterization, and antiproliferative evaluation of novel sorafenib analogs for the treatment of hepatocellular carcinoma.\",\"authors\":\"Marwan Imad Jihad, Monther Faisal Mahdi\",\"doi\":\"10.4103/JAPTR.JAPTR_282_23\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Cancer is a disease triggered by an uncontrolled proliferation of a cluster of cells, typically originating from a single cell. Sorafenib, a widely utilized pharmaceutical, has limitations in clinical use due to pharmacokinetic challenges and the development of resistance mechanisms. This investigation aimed to synthesize new sorafenib analogs and evaluated their activity against HepG2 cell lines, specifically targeting hepatocellular carcinoma (HCC). Seven sorafenib analogs were synthesized and identified by Fourier-transform infrared spectroscopy and 1H-NMR spectra. Cytotoxicity of the analogs was assessed on the human HepG2 cancer cell line by (3-(4, 5-dimethylthazolk-2-yl)-2, 5-diphenyl tetrazolium bromide) colorimetric assay. Results revealed that among the studied compounds, 4b exhibited the most pronounced cytotoxicity against cancer cells, surpassing even the efficacy of sorafenib. This suggested that small substitutions on the NH moiety play a crucial role in the activity against the human HepG2 liver cancer cell line. These findings provide valuable insights for the development of potential anticancer-targeting HCC.</p>\",\"PeriodicalId\":14877,\"journal\":{\"name\":\"Journal of Advanced Pharmaceutical Technology & Research\",\"volume\":\"14 3\",\"pages\":\"274-279\"},\"PeriodicalIF\":1.4000,\"publicationDate\":\"2023-07-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/e4/c3/JAPTR-14-274.PMC10483918.pdf\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Advanced Pharmaceutical Technology & Research\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.4103/JAPTR.JAPTR_282_23\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2023/7/28 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q3\",\"JCRName\":\"Pharmacology, Toxicology and Pharmaceutics\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Advanced Pharmaceutical Technology & Research","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.4103/JAPTR.JAPTR_282_23","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2023/7/28 0:00:00","PubModel":"Epub","JCR":"Q3","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
Synthesis, characterization, and antiproliferative evaluation of novel sorafenib analogs for the treatment of hepatocellular carcinoma.
Cancer is a disease triggered by an uncontrolled proliferation of a cluster of cells, typically originating from a single cell. Sorafenib, a widely utilized pharmaceutical, has limitations in clinical use due to pharmacokinetic challenges and the development of resistance mechanisms. This investigation aimed to synthesize new sorafenib analogs and evaluated their activity against HepG2 cell lines, specifically targeting hepatocellular carcinoma (HCC). Seven sorafenib analogs were synthesized and identified by Fourier-transform infrared spectroscopy and 1H-NMR spectra. Cytotoxicity of the analogs was assessed on the human HepG2 cancer cell line by (3-(4, 5-dimethylthazolk-2-yl)-2, 5-diphenyl tetrazolium bromide) colorimetric assay. Results revealed that among the studied compounds, 4b exhibited the most pronounced cytotoxicity against cancer cells, surpassing even the efficacy of sorafenib. This suggested that small substitutions on the NH moiety play a crucial role in the activity against the human HepG2 liver cancer cell line. These findings provide valuable insights for the development of potential anticancer-targeting HCC.
期刊介绍:
Journal of Advanced Pharmaceutical Technology & Research (JAPTR) is an Official Publication of Society of Pharmaceutical Education & Research™. It is an international journal published Quarterly. Journal of Advanced Pharmaceutical Technology & Research (JAPTR) is available in online and print version. It is a peer reviewed journal aiming to communicate high quality original research work, reviews, short communications, case report, Ethics Forum, Education Forum and Letter to editor that contribute significantly to further the scientific knowledge related to the field of Pharmacy i.e. Pharmaceutics, Pharmacology, Pharmacognosy, Pharmaceutical Chemistry. Articles with timely interest and newer research concepts will be given more preference.