Discovery of a more potent anticancer agent than C4-benzazole 1,8-naphthalimide derivatives against murine melanoma

doi:10.1002/jccs.202000019

淡江大學機構典藏 > 理學院 > 應用科學博士班 > 期刊論文 > Item 987654321/118898

jsp.display-item.identifier=請使用永久網址來引用或連結此文件: https://tkuir.lib.tku.edu.tw/dspace/handle/987654321/118898

题名:	Discovery of a more potent anticancer agent than C4-benzazole 1,8-naphthalimide derivatives against murine melanoma
作者:	Chi-Hua Tung;Yen-Ta Lu;Wei-Ting Kao;Jen-Wei Liu;Yi-Hsuan Lai;Shinn-Jong Jiang;Hao-Ping Chen;Tzenge-Lien Shih
日期:	2020-06-24
上传时间:	2020-07-13 12:10:27 (UTC+8)
摘要:	Three novel naphthalimide‐based derivatives were synthesized and tested in vitro as anticancer agents. Our previous report of the C4‐benzazole 1,8‐naphthalimide derivatives showed good inhibition against murine melanoma. We aimed to synthesize more potent agents and found that compound 5 reported in this article behaved 5‐ to 10‐fold potency than our previous best results. The unique structure of compound 5 consisted of a naphthalimide framework in which C4 position was linked with an ethylenediamine group where the amino group was coupled with a 2‐piconic acid moiety. Compound 5 exhibited the most potent inhibitory activity toward human DNA topoisomerase II proteins with IC50 value (2.6 ± 0.1 μM) against murine B16F10 melanoma cells among the three target compounds synthesized in this study. In accordance with this finding, the results of molecular docking also revealed that compound 5 has the highest affinity with human DNA topoisomerase II among the selected compounds. Compound 5 , therefore, has high potential for becoming a lead compound.
關聯:	Journal of the Chinese Chemical Society 67(7), p.1254-1262
DOI:	10.1002/jccs.202000019
显示于类别:	[應用科學博士班] 期刊論文

文件中的档案:

档案	描述	大小	格式	浏览次数
index.html		0Kb	HTML	266	检视/开启

在機構典藏中所有的数据项都受到原著作权保护.

TAIR相关文章

数据加载中.....