Abstract：2-Fluoro-6-morpholinobenzonitrile(1) was prepared by reaction of 2,6-difluorobenzonitrile with morpholine. 4-Morpholino-1H-indazol-3-amine(2) was synthesized by cyclization of 1 with hydrazine. 2 was coupled with various carboxylic acids to afford eight novel indazole derivatives(4a~4h). The structures were characterized by 1H NMR， IR and HR-ESI-MS. The antitumor activities were investigated. The results showed that 4-(4-methylpiperazin-1-yl)-N-(4-morpholino-1H-indazol-3-yl)-4-oxobutanamide(〖WTHZ〗〖STHZ〗4a〖STBZ〗〖WTBZ〗) exhibited potent antitumor activities against K-562, SMMC7721 and T-47D tumor cell lines with IC50 of 0.056 μmol·L-1 , 0.062 μmol·L-1 and 0.086 μmol·L-1, respectively.
周云鹏, 何畅, 宋端正, 陈烨, 刘举, 张秋实, 王洋. 新型吲唑类化合物的合成及其抗肿瘤活性[J]. 合成化学, 2016, 24(4): 293-296.
ZHOU Yun-peng, HE Chang, SONG Duan-zheng, CHEN Ye, LIU Ju, ZHANG Qiu-shi, WANG Yang. Synthesis and Antitumor Activities of Novel Indazole Derivatives. Chinese Journal of Synthetic Chemistry, 2016, 24(4): 293-296.
2016, Vol. 24 
