Synthesis, anticancer and antibacterial activity of salinomycin N-benzyl amides.
Synthesis, anticancer and antibacterial activity of salinomycin N-benzyl amides.
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DOI：
10.3390/molecules191219435
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发表时间：
2014-11-25
期刊：
影响因子：
--
通讯作者：
Huczyński A
中科院分区：
文献类型：
--
作者：
Antoszczak M;Maj E;Napiórkowska A;Stefańska J;Augustynowicz-Kopeć E;Wietrzyk J;Janczak J;Brzezinski B;Huczyński A
首次合成了12个新的单取代N-苄基盐霉素酰胺类化合物（SAL），并用NMR和FT-IR等方法对其结构进行了表征。用单晶X-射线衍射法测定了三种盐霉素衍生物的固态分子结构。筛选获得的所有化合物对各种人类癌细胞系以及对最有问题的细菌菌株如耐甲氧西林金黄色葡萄球菌（MRSA）和表皮葡萄球菌（MRSE）以及结核分枝杆菌的抗增殖活性。新型盐霉素衍生物对耐药细胞系表现出有效的抗癌活性。此外，盐霉素的两个N-苄基酰胺显示出有趣的抗菌活性。最具活性的是-邻位取代的SAL的N-苄基酰胺，最不具抗癌活性的是-帕拉取代的SAL衍生物。
A series of 12 novel monosubstituted N-benzyl amides of salinomycin (SAL) was synthesized for the first time and characterized by NMR and FT-IR spectroscopic methods. Molecular structures of three salinomycin derivatives in the solid state were determined using single crystal X-ray method. All compounds obtained were screened for their antiproliferative activity against various human cancer cell lines as well as against the most problematic bacteria strains such as methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE), and Mycobacterium tuberculosis. Novel salinomycin derivatives exhibited potent anticancer activity against drug-resistant cell lines. Additionally, two N-benzyl amides of salinomycin revealed interesting antibacterial activity. The most active were N-benzyl amides of SAL substituted at -ortho position and the least anticancer active derivatives were those substituted at the -para position.
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影响因子：
1.8
作者：
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通讯作者：
Sikorski, Artur
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影响因子：
6.3
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通讯作者：
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影响因子：
64.5
作者：
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通讯作者：
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