Chinese Journal of Organic Chemistry >
Synthesis and Cytotoxicity of N12-Ethyl Substituted Indolocarbazole Derivatives
Received date: 2016-02-29
Revised date: 2016-04-17
Online 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 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
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
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