Citation: Ma Hongguang, Wang Liping, Xu Zhihong, Zhang Yapeng, Li Xia, Zhu Weiming. Synthesis and Cytotoxicity of N₁₂-Ethyl Substituted Indolocarbazole Derivatives[J]. Chinese Journal of Organic Chemistry, ;2016, 36(8): 1839-1846. doi: 10.6023/cjoc201602035 shu

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

Corresponding author: Zhu Weiming, weimingzhu@ouc.edu.cn
Received Date: 29 February 2016
Revised Date: 17 April 2016

Fund Project: Project supported by the National Natural Science Foundation of China Nos. 81561148012，41376148，81273532，30973680and the National Natural Science Foundation of China-Guangdong Fund Joint Project No. U1501221the National High-Tech R & D Program of China No. 2012AA092104

Figures(1)

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.
- N₁₂-ethyl indolocarbazole,
- synthesis,
- cytotoxicity
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Synthesis and Cytotoxicity of N₁₂-Ethyl Substituted Indolocarbazole Derivatives