Synthesis of novel benzofluorenone derivatives and their HIV reverse transcriptase inhibitory activity

T. Lambat, S. Deo
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引用次数: 8

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).
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新型苯并芴酮衍生物的合成及其HIV逆转录酶抑制活性
通过β-芳烯基-β-苯甲酰丙酸分子内环化制备了新型苯芴酮衍生物,收率非常高。在100℃条件下,用极少量的K10蒙脱土作为非均相催化剂,在乙醇介质中有效地促进了反应。这些新合成的苯并芴酮衍生物首次显示出抗hiv(抗逆转录病毒)活性。这种重要的活性是通过使用常规检测试剂盒来估计的。此外,在所合成的碱式苯芴酮衍生物中,化合物2C的IC50最低(21.86µg/mL),其次是化合物2G, IC50最低(27.40µg/mL)。
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