Synthesis and Cytotoxicity of N12-Ethyl Substituted Indolocarbazole Derivatives

doi:10.6023/cjoc201602035

Chin. J. Org. Chem. ›› 2016, Vol. 36 ›› Issue (8): 1839-1846.DOI: 10.6023/cjoc201602035 Previous Articles Next Articles

ARTICLE

N₁₂-乙基取代吲哚咔唑衍生物的合成及细胞毒活性研究

马红光^a, 王立平^b, 徐志红^a, 张亚鹏^a, 李霞^c, 朱伟明^a

a 中国海洋大学医药学院海洋药物教育部重点实验室青岛 266003;
b 贵州省中国科学院天然产物化学重点实验室贵阳 550002;
c 山东大学威海校区海洋学院威海 264209

收稿日期:2016-02-29 修回日期:2016-04-17 发布日期:2016-05-03
通讯作者: 朱伟明 E-mail:weimingzhu@ouc.edu.cn
基金资助:
国家自然科学基金（Nos. 81561148012，41376148，81273532，30973680）、高科技发展计划（No. 2012AA092104）以及国家自然科学基金-广东联合基金（No. U1501221）资助项目.

Synthesis and Cytotoxicity of N₁₂-Ethyl Substituted Indolocarbazole Derivatives

Ma Hongguang^a, Wang Liping^b, Xu Zhihong^a, Zhang Yapeng^a, Li Xia^c, Zhu Weiming^a

a Key Laboratory of Marine Drugs, Ministry Education of China, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003;
b Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, Guiyang 550002;
c School of Ocean, Shandong University, Weihai 264209

Received:2016-02-29 Revised:2016-04-17 Published:2016-05-03
Supported by:
Project supported by the National Natural Science Foundation of China (Nos. 81561148012, 41376148, 81273532, 30973680), the National High-Tech R&D Program of China (No. 2012AA092104), and the National Natural Science Foundation of China-Guangdong Fund Joint Project (No. U1406402).

1. Synthesis and Cytotoxicity of N₁₂-Ethyl Substituted Indolocarbazole Derivatives.PDF(2408KB)

Abstract

Nine new N₁₂-ethyl substituted indolocarbazole derivatives were synthesized. Their structures were identified by ¹H NMR, ¹³C NMR and HRESIMS. The thiazolyl blue tetrazolium bromide (MTT) method was used to evaluate the cytotoxicities of these derivatives against A549, HepG-2 and Hela cell lines, while the cell counting kit-8 (CCK-8) method was used to evaluate cytotoxicity against K562 cell lines. The results showed that compounds 7～9 displayed comparable cytotoxicity to adriamycin (ADM) against K562 cell lines with the IC₅₀ values of 0.43～0.93 μmol/L. Compounds 8 and 12 showed comparable cytotoxicity to ADM against Hela cell lines with the IC₅₀ values of 1.23 and 0.43 μmol/L, respectively. The hydrochloride 14 of compound 13 exhibited good cytotoxicity against the four cell lines with the IC₅₀ values of 0.23～1.72 μmol/L, indicating a worth of further study as an antitumor lead compound.

Key words: N₁₂-ethyl indolocarbazole, synthesis, cytotoxicity

Cite this article

Ma Hongguang, Wang Liping, Xu Zhihong, Zhang Yapeng, Li Xia, Zhu Weiming. Synthesis and Cytotoxicity of N₁₂-Ethyl Substituted Indolocarbazole Derivatives[J]. Chin. J. Org. Chem., 2016, 36(8): 1839-1846.

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N₁₂-乙基取代吲哚咔唑衍生物的合成及细胞毒活性研究

Synthesis and Cytotoxicity of N₁₂-Ethyl Substituted Indolocarbazole Derivatives

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N12-乙基取代吲哚咔唑衍生物的合成及细胞毒活性研究