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Anticancer and Tubulin Polymerisation Inhibition Activity of Benzylidene Indanones and Process of Preparing the Same

机译:亚苄基茚满酮的抗癌和微管蛋白聚合抑制活性及其制备方法

摘要

The present invention relates to benzylidene indanones of general formula 1. The compounds exhibited tubulin polymerisation inhibition. A series of compounds 2-benzylidene 3-(3,4,5-trimethoxyphenyl) indanones having general formulae 1 were synthesized from gallic acid through a chemical process. 2-(3,4-Methylenedioxybenzylidine), 3-(3,4,5-trimethoxyphenyl), 4,5,6-trimethoxyindanone (8), a representative compound of this series possessing the molecular formulae C29H28O9, was synthesized from gallic acid and exhibits potent anticancer activity. Compound 8 was evaluated for acute oral activity in Swiss albino mice and found to be safe up to 300 mg/kg body weight. The anticancer activity of the compounds has been determined, in order to obtain new potent and cost effective molecules using an in vitro cytotoxicity assay.; embedded image
机译:本发明涉及通式1的亚苄基茚满酮。该化合物表现出微管蛋白聚合抑制作用。由没食子酸通过化学方法合成了一系列通式为 1 的2-亚苄基3-(3,4,5-三甲氧基苯基)茚满酮。 2-(3,4-亚甲基二氧基苄基),3-(3,4,5-三甲氧基苯基),4,5,6-三甲氧基茚满(8),该系列的代表性化合物,具有分子式C 29 H 28 O 9 是由没食子酸合成的,具有很强的抗癌活性。评估了化合物8在瑞士白化病小鼠中的急性口服活性,发现在300 mg / kg体重以下是安全的。已经确定了化合物的抗癌活性,以便使用体外细胞毒性测定法获得新的有效且具有成本效益的分子。 “嵌入式图像”

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