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



马红光a, 王立平b, 徐志红a, 张亚鹏a, 李霞c, 朱伟明a   

  1. 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
  • 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 Hongguanga, Wang Lipingb, Xu Zhihonga, Zhang Yapenga, Li Xiac, Zhu Weiminga   

  1. 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).

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 79 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