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| Synthesis and Antitumor Activities of Novel Indazole Derivatives |
| ZHOU Yun-peng, HE Chang, SONG Duan-zheng, CHEN Ye, LIU Ju, ZHANG Qiu-shi, WANG Yang |
| New Drug Research and Development Key Laboratory of Liaoning Province, College of Pharmacy, Liaoning Uninversity, Shenyang 110036, China |
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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.
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Received: 13 January 2016
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2016, Vol. 24 
