ZHOU Hao, ZHOU Feng, ZHOU Youjun. Design, synthesis and anti-tumor activities in vitro of novel 3-substituted indolin-2-one compounds[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(2): 131-133,142. doi: 10.3969/j.issn.1006-0111.2015.02.010
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ZHOU Hao, ZHOU Feng, ZHOU Youjun. Design, synthesis and anti-tumor activities in vitro of novel 3-substituted indolin-2-one compounds[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(2): 131-133,142. doi: 10.3969/j.issn.1006-0111.2015.02.010
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Design, synthesis and anti-tumor activities in vitro of novel 3-substituted indolin-2-one compounds
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Department of Medical Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
- Received Date: 2014-11-03
- Rev Recd Date:
2015-01-20
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Abstract
Objective To compose and evaluate anti-tumor activities of 3-substituted indole-2-one compounds which may have dual inhibitory activities against both tubulin protein and VEGFR-2 tyrosine kinase. Methods Target compounds were prepared starting from substituted aniline via condensation, cyclization and reduction. Results 11 target compounds were synthesized and all the compounds displayed moderate anti-proliferative activities against three tumor cell lines. Compound j9 showed a certain inhibitory activity against both VEGFR-2 kinase and tubulin protein in vitro. Conclusion This series of indolin-2-one derivatives were found to be a novel kind of multi-target inhibitor.
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