Uttara Soumyanarayanan, Varadaraj G Bhat, Sidhartha S Kar, Jesil A Mathew
{"title":"Monastrol模拟Biginelli二氢嘧啶衍生物的合成、对HepG2和HeLa细胞株的细胞毒性筛选及分子模拟研究","authors":"Uttara Soumyanarayanan, Varadaraj G Bhat, Sidhartha S Kar, Jesil A Mathew","doi":"10.1186/2191-2858-2-23","DOIUrl":null,"url":null,"abstract":"<p><p> Biginelli dihydropyrimidinone derivatives as structural analogs of monastrol, a known human kinesin Eg5 inhibitor, were synthesized. IC50 values of the synthesized compounds against the proliferation of human hepatocellular carcinoma and human epithelial carcinoma cell lines were determined through MTT assay. Molecular docking study gave a clear insight into the structural activity relationship of the compounds in comparison with monastrol.</p>","PeriodicalId":19639,"journal":{"name":"Organic and Medicinal Chemistry Letters","volume":"2 1","pages":"23"},"PeriodicalIF":0.0000,"publicationDate":"2012-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1186/2191-2858-2-23","citationCount":"35","resultStr":"{\"title\":\"Monastrol mimic Biginelli dihydropyrimidinone derivatives: synthesis, cytotoxicity screening against HepG2 and HeLa cell lines and molecular modeling study.\",\"authors\":\"Uttara Soumyanarayanan, Varadaraj G Bhat, Sidhartha S Kar, Jesil A Mathew\",\"doi\":\"10.1186/2191-2858-2-23\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p> Biginelli dihydropyrimidinone derivatives as structural analogs of monastrol, a known human kinesin Eg5 inhibitor, were synthesized. IC50 values of the synthesized compounds against the proliferation of human hepatocellular carcinoma and human epithelial carcinoma cell lines were determined through MTT assay. Molecular docking study gave a clear insight into the structural activity relationship of the compounds in comparison with monastrol.</p>\",\"PeriodicalId\":19639,\"journal\":{\"name\":\"Organic and Medicinal Chemistry Letters\",\"volume\":\"2 1\",\"pages\":\"23\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2012-06-12\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1186/2191-2858-2-23\",\"citationCount\":\"35\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Organic and Medicinal Chemistry Letters\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1186/2191-2858-2-23\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Organic and Medicinal Chemistry Letters","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1186/2191-2858-2-23","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Monastrol mimic Biginelli dihydropyrimidinone derivatives: synthesis, cytotoxicity screening against HepG2 and HeLa cell lines and molecular modeling study.
Biginelli dihydropyrimidinone derivatives as structural analogs of monastrol, a known human kinesin Eg5 inhibitor, were synthesized. IC50 values of the synthesized compounds against the proliferation of human hepatocellular carcinoma and human epithelial carcinoma cell lines were determined through MTT assay. Molecular docking study gave a clear insight into the structural activity relationship of the compounds in comparison with monastrol.