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Synthesis and Antitumor Activity of Sorafenib Analogs Containing a Tetrazole Moiety |
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| Authors: | TIAN Ye YU Simiao CAI Lude GONG Guowei WU Guodong QI Hongxia ZHAO Yanfang QIN Mingze |
| Affiliation: | 1. Key Laboratory of Structure-based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China; 2. Department of Bioengineering, Zhuhai Campus of Zunyi Medical University, Zhuhai 519041, P. R. China; 3. Shengjing Hospital of China Medical University, Shenyang 110016, P. R. China |
| Abstract: | A novel series of diaryl biuret derivatives containing a tetrazole moiety was designed and synthesized. All the target compounds were evaluated for their in vitro antitumor activity against HT-29, HepG2, MCF-7 and A549 cells by MTT assay. Most of them exhibited obvious antitumor activity, and four of them (4a, 4c, 4h and 7a) were superior to sorafenib in general. Among them, Compound 4h displayed more potent activity than sorafenib in all tested cancer cells. Compound 4c exhibited the most outstanding activity in inhibition of growth of HepG2 cells (IC50=0.55 μmol/L). Further, they both revealed favorable metabolic stability in in vitro assay. Compounds 4c and 4h are promising candidates for further development. |
| Keywords: | Sorafenib derivative Tetrazole moiety Antitumor activity |
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