{"title":"新型苯并芴酮衍生物的合成及其HIV逆转录酶抑制活性","authors":"T. Lambat, S. Deo","doi":"10.1080/22243682.2016.1251334","DOIUrl":null,"url":null,"abstract":"Novel benzofluorenone derivatives have been prepared in remarkably outstanding yield through intramolecular cyclization of β-arylidene-β-benzoylpropionic acid. The reaction was promoted proficiently by extremely small amounts of montmorillonite K10 acting as a heterogeneous catalyst using ethanolic medium at 100 °C. It is for the first time that, these newly synthesized benzofluorenone derivatives exhibited anti-HIV (antiretroviral) activity. This important activity was estimated by using regular assay kits. Further, among the synthesized basic benzofluorenone derivatives, the compound named ‘2C’ was found to be most potent with the lowest IC50 (21.86 µg/mL) followed by the compound ‘2G’ with IC50 (27.40 µg/mL).","PeriodicalId":17291,"journal":{"name":"Journal of the Chinese Advanced Materials Society","volume":"44 1","pages":"20-32"},"PeriodicalIF":0.0000,"publicationDate":"2017-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"8","resultStr":"{\"title\":\"Synthesis of novel benzofluorenone derivatives and their HIV reverse transcriptase inhibitory activity\",\"authors\":\"T. Lambat, S. Deo\",\"doi\":\"10.1080/22243682.2016.1251334\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Novel benzofluorenone derivatives have been prepared in remarkably outstanding yield through intramolecular cyclization of β-arylidene-β-benzoylpropionic acid. The reaction was promoted proficiently by extremely small amounts of montmorillonite K10 acting as a heterogeneous catalyst using ethanolic medium at 100 °C. It is for the first time that, these newly synthesized benzofluorenone derivatives exhibited anti-HIV (antiretroviral) activity. This important activity was estimated by using regular assay kits. Further, among the synthesized basic benzofluorenone derivatives, the compound named ‘2C’ was found to be most potent with the lowest IC50 (21.86 µg/mL) followed by the compound ‘2G’ with IC50 (27.40 µg/mL).\",\"PeriodicalId\":17291,\"journal\":{\"name\":\"Journal of the Chinese Advanced Materials Society\",\"volume\":\"44 1\",\"pages\":\"20-32\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2017-01-02\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"8\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of the Chinese Advanced Materials Society\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1080/22243682.2016.1251334\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of the Chinese Advanced Materials Society","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1080/22243682.2016.1251334","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis of novel benzofluorenone derivatives and their HIV reverse transcriptase inhibitory activity
Novel benzofluorenone derivatives have been prepared in remarkably outstanding yield through intramolecular cyclization of β-arylidene-β-benzoylpropionic acid. The reaction was promoted proficiently by extremely small amounts of montmorillonite K10 acting as a heterogeneous catalyst using ethanolic medium at 100 °C. It is for the first time that, these newly synthesized benzofluorenone derivatives exhibited anti-HIV (antiretroviral) activity. This important activity was estimated by using regular assay kits. Further, among the synthesized basic benzofluorenone derivatives, the compound named ‘2C’ was found to be most potent with the lowest IC50 (21.86 µg/mL) followed by the compound ‘2G’ with IC50 (27.40 µg/mL).