Chandrabose Karthikeyan , Viswas Raja Solomon , Hoyun Lee , Piyush Trivedi
{"title":"一些isatin-linked chalcones作为新型抗乳腺癌药物的设计、合成和生物学评价:分子杂交方法","authors":"Chandrabose Karthikeyan , Viswas Raja Solomon , Hoyun Lee , Piyush Trivedi","doi":"10.1016/j.bionut.2013.04.001","DOIUrl":null,"url":null,"abstract":"<div><p><span><span><span>Isatins are endogenous molecules present in human and mammals which exhibits diverse pharmacological profiles including </span>anticancer activity. Similarly, </span>chalcones<span>, which are common substructures in numerous natural products belonging to the flavonoid<span> family, show potent anticancer properties. A novel series of 3-(2-oxo-2-phenylethylidene)indolin-2-ones incorporating pharmacophoric elements of isatins and chalcones were designed and synthesized. The compounds were evaluated for anticancer activity against three breast cancer cell lines. Most of the compounds showed promising anticancer activity (<</span></span></span> <!-->20<!--> <!-->μM) against the studied cell lines. Compound <strong>2c</strong>, bearing a 5-chloro substituent in the benzo ring of the isatin moiety and 3,4-dimethoxy substitutions in the phenyl ring, was found to be the most active in the series with GI<sub>50</sub><span> values of 8.54, 4.76 and 3.59 against MDA-MB231, MDA-MB468 and MCF7 cells, respectively. Overall, the findings of the study highlight 3-(2-oxo-2-phenylethylidene)indolin-2-one as a potential new lead in the search of drugs<span> for the treatment of breast cancer.</span></span></p></div>","PeriodicalId":100182,"journal":{"name":"Biomedicine & Preventive Nutrition","volume":"3 4","pages":"Pages 325-330"},"PeriodicalIF":0.0000,"publicationDate":"2013-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.bionut.2013.04.001","citationCount":"47","resultStr":"{\"title\":\"Design, synthesis and biological evaluation of some isatin-linked chalcones as novel anti-breast cancer agents: A molecular hybridization approach\",\"authors\":\"Chandrabose Karthikeyan , Viswas Raja Solomon , Hoyun Lee , Piyush Trivedi\",\"doi\":\"10.1016/j.bionut.2013.04.001\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p><span><span><span>Isatins are endogenous molecules present in human and mammals which exhibits diverse pharmacological profiles including </span>anticancer activity. Similarly, </span>chalcones<span>, which are common substructures in numerous natural products belonging to the flavonoid<span> family, show potent anticancer properties. A novel series of 3-(2-oxo-2-phenylethylidene)indolin-2-ones incorporating pharmacophoric elements of isatins and chalcones were designed and synthesized. The compounds were evaluated for anticancer activity against three breast cancer cell lines. Most of the compounds showed promising anticancer activity (<</span></span></span> <!-->20<!--> <!-->μM) against the studied cell lines. Compound <strong>2c</strong>, bearing a 5-chloro substituent in the benzo ring of the isatin moiety and 3,4-dimethoxy substitutions in the phenyl ring, was found to be the most active in the series with GI<sub>50</sub><span> values of 8.54, 4.76 and 3.59 against MDA-MB231, MDA-MB468 and MCF7 cells, respectively. Overall, the findings of the study highlight 3-(2-oxo-2-phenylethylidene)indolin-2-one as a potential new lead in the search of drugs<span> for the treatment of breast cancer.</span></span></p></div>\",\"PeriodicalId\":100182,\"journal\":{\"name\":\"Biomedicine & Preventive Nutrition\",\"volume\":\"3 4\",\"pages\":\"Pages 325-330\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2013-10-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/j.bionut.2013.04.001\",\"citationCount\":\"47\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Biomedicine & Preventive Nutrition\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S2210523913000251\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Biomedicine & Preventive Nutrition","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S2210523913000251","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Design, synthesis and biological evaluation of some isatin-linked chalcones as novel anti-breast cancer agents: A molecular hybridization approach
Isatins are endogenous molecules present in human and mammals which exhibits diverse pharmacological profiles including anticancer activity. Similarly, chalcones, which are common substructures in numerous natural products belonging to the flavonoid family, show potent anticancer properties. A novel series of 3-(2-oxo-2-phenylethylidene)indolin-2-ones incorporating pharmacophoric elements of isatins and chalcones were designed and synthesized. The compounds were evaluated for anticancer activity against three breast cancer cell lines. Most of the compounds showed promising anticancer activity (< 20 μM) against the studied cell lines. Compound 2c, bearing a 5-chloro substituent in the benzo ring of the isatin moiety and 3,4-dimethoxy substitutions in the phenyl ring, was found to be the most active in the series with GI50 values of 8.54, 4.76 and 3.59 against MDA-MB231, MDA-MB468 and MCF7 cells, respectively. Overall, the findings of the study highlight 3-(2-oxo-2-phenylethylidene)indolin-2-one as a potential new lead in the search of drugs for the treatment of breast cancer.