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一些新型1-吡啶甲酰基-4-取代硫代氨基脲衍生物的合成、抗菌及抗增殖潜力

Synthesis, antibacterial and antiproliferative potential of some new 1-pyridinecarbonyl-4-substituted thiosemicarbazide derivatives.

作者信息

Pitucha Monika, Woś Maciej, Miazga-Karska Malgorzata, Klimek Katarzyna, Mirosław Barbara, Pachuta-Stec Anna, Gładysz Agata, Ginalska Grazyna

机构信息

Department of Organic Chemistry, Medical University, Chodzki 4A, 20-093 Lublin, Poland.

Chair and Department of Biochemistry and Biotechnology, Medical University, Chodzki 1, 20-093 Lublin, Poland.

出版信息

Med Chem Res. 2016;25:1666-1677. doi: 10.1007/s00044-016-1599-6. Epub 2016 Jun 1.

DOI:10.1007/s00044-016-1599-6
PMID:27499604
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4958397/
Abstract

In this study, the antibacterial, cytotoxic and antiproliferative activities of novel thiosemicarbazide derivatives were assessed. Our results demonstrated that some of the novel compounds possess good antibacterial properties against , and and are only slightly cytotoxic; thus, they exhibit an excellent therapeutic index, which is higher than that of ethacridine lactate. Moreover, our data showed that compounds and have an antiproliferative activity against human breast adenocarcinoma and human hepatocellular carcinoma cell lines. We expect that the novel thiosemicarbazide derivatives can be used as agents for treatment of dental caries and also for chemotherapy support.

摘要

在本研究中,对新型硫代氨基脲衍生物的抗菌、细胞毒性和抗增殖活性进行了评估。我们的结果表明,一些新型化合物对[具体细菌名称1]、[具体细菌名称2]和[具体细菌名称3]具有良好的抗菌性能,且细胞毒性轻微;因此,它们具有优异的治疗指数,高于乳酸依沙吖啶。此外,我们的数据显示化合物[化合物编号1]和[化合物编号2]对人乳腺腺癌和人肝癌细胞系具有抗增殖活性。我们期望新型硫代氨基脲衍生物可作为治疗龋齿的药物,也可用于化疗辅助。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7050/4958397/f3829847f072/44_2016_1599_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7050/4958397/bcab652f406b/44_2016_1599_Sch1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7050/4958397/9f756ce9c18f/44_2016_1599_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7050/4958397/ba23d2bbdd67/44_2016_1599_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7050/4958397/1c26e480fe7a/44_2016_1599_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7050/4958397/f3829847f072/44_2016_1599_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7050/4958397/bcab652f406b/44_2016_1599_Sch1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7050/4958397/9f756ce9c18f/44_2016_1599_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7050/4958397/ba23d2bbdd67/44_2016_1599_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7050/4958397/1c26e480fe7a/44_2016_1599_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7050/4958397/f3829847f072/44_2016_1599_Fig4_HTML.jpg

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