Synthesis and Bioevaluation of Shikonin Derivatives

被引：4
作者：
Cao, Sufen [1 ]
Zhang, Jiangang [2 ]
Duan, Wenhu [1 ,2 ]
机构：
[1] East China Univ Sci & Technol, Sch Pharm, Dept Pharmaceut Sci, Shanghai, Peoples R China
[2] Chinese Acad Sci, Shanghai Inst Materia Med, Dept Med Chem, Shanghai 201203, Peoples R China
来源：
LETTERS IN DRUG DESIGN & DISCOVERY | 2018年 / 15卷 / 09期
基金：
中国国家自然科学基金;
关键词：
Amidation; chemical stability; cytotoxicity; esterification; shikonin derivatives; synthesis; SRB assay; cell lines; ANTITUMOR-ACTIVITY; BETA-HYDROXYISOVALERYLSHIKONIN; LITHOSPERMUM-ERYTHRORHIZON; BIOLOGICAL EVALUATION; IN-VIVO; ALKANNIN; INHIBIT; INDUCTION; DESIGN; GROWTH;
D O I：
10.2174/1570180815666171229152139
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Background: Ester and amide derivatives of shikonin were synthesized to improve the chemical stability of shikonin. Methods: All synthesized compounds were evaluated for their antiproliferative activity against A549 cell line by SRB assay, and five of them demonstrated comparable cytotoxicity to shikonin. Results and Conclusion: The most potent compound, 22d, was more stable and potent than shikonin.
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收藏
页码：945 / 950
页数：6
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