Synthesis, characterization, in vitro SAR study, and preliminary in vivo toxicity evaluation of naphthylmethyl substituted bis-imidazolium salts.
Synthesis, characterization, in vitro SAR study, and preliminary in vivo toxicity evaluation of naphthylmethyl substituted bis-imidazolium salts.
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DOI：
10.1016/j.bmc.2020.115893
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发表时间：
2021-01-15
影响因子：
3.5
通讯作者：
Youngs WJ
中科院分区：
文献类型：
--
作者：
Southerland MR;DeBord MA;Johnson NA;Crabtree SR;Alexander NE;Stromyer ML;Wagers PO;Panzner MJ;Wesdemiotis C;Shriver LP;Tessier CA;Youngs WJ
合成了一系列新型双咪唑鎓盐，并对其进行了表征，并在体外对一组非小细胞肺癌（NSCLC）细胞进行了评价。将两个咪唑鎓核与不同长度的烷基链连接，建立构效关系（SAR）。增加连接烷基链的长度显示与抗增殖活性的增加相关。国家癌症研究所的NCI-60人类肿瘤细胞系筛选证实了这一趋势。选择含有癸基接头链的化合物10用于C578 BL/6小鼠的进一步体内毒性研究。小鼠对该化合物耐受良好，所有动物均存活，并在研究过程中体重增加。
A series of novel bis-imidazolium salts was synthesized, characterized, and evaluated in vitro against a panel of non-small cell lung cancer (NSCLC) cells. Two imidazolium cores were connected with alkyl chains of varying lengths to develop a structure activity relationship (SAR). Increasing the length of the connecting alkyl chain was shown to correlate to an increase in the anti-proliferative activity. The National Cancer Institute’s NCI-60 human tumor cell line screen confirmed this trend. The compound containing a decyl linker chain, 10, was chosen for further in vivo toxicity studies with C578BL/6 mice. The compound was well tolerated by the mice and all of the animals survived and gained weight over the course of the study.
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5.1
作者：
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通讯作者：
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通讯作者：
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