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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and anticancer activity evaluation of 4-thiazolidinones containing benzothiazole moiety.
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Synthesis and anticancer activity evaluation of 4-thiazolidinones containing benzothiazole moiety.

机译：含苯并噻唑部分的4-噻唑烷酮的合成与抗癌活性评价。

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摘要

Antitumor screening of several novel 4-thiazolidinones with benzothiazole moiety has been performed. Reactions of (benzothiazole-2-yl)hydrazine with trithiocarbonyl diglycolic acid or 6-methyl-2-aminobenzothiazole with 2-carbethoxymethylthio-2-thiazoline-4-one have yielded starting 3- (1) or 2-substituted (11) 4-thiazolidinones which have been subsequently utilized in a Knoevenagel condensation for obtaining a series of 5-arylidene derivatives 2-10, 12-16. Compound 11 has been obtained alternatively by a counter synthesis method based on the reaction of 2-chloro-N-(6-methylbenzothiazol-2-yl)-acetamide and ammonium thiocyanate. The structures of compounds have been determined by (1)H, (13)C NMR, IR and X-ray analysis. In vitro anticancer activity of the synthesized compounds was tested by the National Cancer Institute and two (6, 16) of them has revealed the anticancer activity on leukemia, melanoma, lung, colon, CNS, ovarian, renal, prostate and breast cancers cell lines. Among tested compounds, 2-{2-[3-(benzothiazol-2-ylamino)-4-oxo-2-thioxothiazolidin-5-ylidenemethyl]-4-chl orophenoxy}-N-(4-methoxyphenyl)-acetamide (6) was found to be the most active candidate with average logGI(50) and logTGI values -5.38 and -4.45 respectively.
机译：抗肿瘤已被执行的几个新的4-噻唑烷酮与苯并噻唑基部分筛选。的（苯并噻唑-2-基）肼与三硫代羰二甘醇酸或6-甲基-2-氨基苯并噻唑与2- carbethoxymethylthio -2-噻唑啉-4-酮已经产生了反应起始物为3-（1）或2-取代的（11）4这已经在Knoevenagel缩合随后被用于获取一系列5-亚芳基衍生物2-10，12-16的-thiazolidinones。化合物11已经由计数器合成方法基于2-氯-N-（6-甲基苯并唑-2-基） - 乙酰胺和硫氰酸铵的反应获得可替换地。化合物的结构已通过（1）H，（13）C NMR，IR和X-射线分析测定。在合成化合物的体外抗癌活性是由美国国家癌症研究所和两个（6，16）的他们已经揭示于白血病，黑色素瘤，肺癌，结肠癌，中枢神经系统癌，卵巢癌，肾癌，前列腺癌和乳腺癌细胞系中的抗癌活性测试。在所测试的化合物，2- {2- [3-（苯并噻唑-2-基氨基）-4-氧代-2-硫代噻唑烷-5-亚基甲基] -4-氯苯氧基CHL} -N-（4-甲氧基苯基） - 乙酰胺（6 ）被发现是最活跃的候选与平均logGI（50）和logTGI值-5.38和-4.45分别。

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