N 12 -乙基取代吲哚咔唑衍生物的合成及细胞毒活性研究

Nine new N12-ethyl substituted indolocarbazole derivatives were synthesized. Their structures were identified by 1 H-NMR, 13 C-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 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.