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Synthesis and antiproliferative activity of salicylidenehydrazones based on indole-2(3)-carboxylic acids
Chemistry of Heterocyclic Compounds ( IF 1.5 ) Pub Date : 2020-07-18 , DOI: 10.1007/s10593-020-02724-2
Andrey G. Vasin , Lyubov G. Dezhenkova , Ivan V. Ivanov , Alexander M. Scherbakov , Andrey E. Shchekotikhin

A series of indole-2(3)-carboxylic acid hydrazones were synthesized and their antiproliferative activity was studied for the K562 leukemia, MCF7 breast adenocarcinoma, and HCT116 colon carcinoma cell lines and resistant HCT116p53KO subline in order to preliminary screen biological properties and to reveal the role of the aldehyde fragment and heterocycle in the ability of compounds to inhibit tumor growth. A number of derivatives have been identified that inhibit the growth of tumor cells in submicromolar concentrations, promising for further optimization and in-depth study of antitumor properties.


中文翻译:

基于吲哚-2(3)-羧酸的水杨基苯并恶唑酮的合成及抗增殖活性

合成了一系列吲哚-2(3)-羧酸,并对其在K562白血病,MCF7乳腺腺癌和HCT116结肠癌细胞系及耐药HCT116p53KO亚系中的抗增殖活性进行了初步筛选,以揭示其生物学特性。醛片段和杂环在化合物抑制肿瘤生长能力中的作用。已经鉴定出许多以亚微摩尔浓度抑制肿瘤细胞生长的衍生物,有望进一步优化和深入研究抗肿瘤特性。
更新日期:2020-07-18
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