新型 1-烷基-3-苯基和 3-烷基-1-苯基咪唑噻唑三嗪的合成及其抗肿瘤活性

IF 16.4 1区化学 Q1 CHEMISTRY, MULTIDISCIPLINARY Accounts of Chemical Research Pub Date : 2024-06-05 DOI:10.1007/s10593-024-03318-y

Alexei N. Izmest’ev, Sergey S. Isakov, Angelina N. Kravchenko, Galina A. Gazieva

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引用次数: 0

摘要

从 1-烷基-3-芳基-4,5-二羟基咪唑啉-2-(硫)-1 中获得了两组异构体咪唑并噻唑并[1,2,4]三嗪及其氧化吲哚亚基衍生物。合成的一种咪唑并[4,5-e]噻唑并[2,3-c][1,2,4]三嗪衍生物在 10 μmol/l 的浓度下对四种肿瘤细胞株具有很高的细胞抑制活性：HL-60（TB）（白血病，生长率-16.1%）、SF-539（中枢神经系统癌症，生长率-2.6%）、MDA-MB-435（黑色素瘤，生长率-21.2%）和 RXF 393（肾癌，生长率-6.1%）。

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The synthesis and antitumor activity of novel 1-alkyl-3-phenyland 3-alkyl-1-phenylimidazothiazolotriazines

Two groups of isomeric imidazothiazolo[1,2,4]triazines and their oxindolylidene derivatives were obtained from 1-alkyl-3-aryl-4,5-dihydroxyimidazolidin-2-(thi)ones. One of the synthesized imidazo[4,5-e]thiazolo[2,3-c][1,2,4]triazine derivatives showed high cytostatic activity at a concentration of 10 μmol/l against four lines of tumor cells: HL-60(TB) (leukemia, –16.1% growth rate), SF-539 (CNS cancer, –2.6% growth rate), MDA-MB-435 (melanoma, –21.2% growth rate), and RXF 393 (kidney cancer, –6.1 % growth rate).

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来源期刊

Accounts of Chemical Research 化学-化学综合

CiteScore

31.40

自引率

1.10%

发文量

312

审稿时长

2 months

期刊介绍： Accounts of Chemical Research presents short, concise and critical articles offering easy-to-read overviews of basic research and applications in all areas of chemistry and biochemistry. These short reviews focus on research from the author’s own laboratory and are designed to teach the reader about a research project. In addition, Accounts of Chemical Research publishes commentaries that give an informed opinion on a current research problem. Special Issues online are devoted to a single topic of unusual activity and significance. Accounts of Chemical Research replaces the traditional article abstract with an article "Conspectus." These entries synopsize the research affording the reader a closer look at the content and significance of an article. Through this provision of a more detailed description of the article contents, the Conspectus enhances the article's discoverability by search engines and the exposure for the research.