Synthesis and antitumor activity of 13-acylmatrine derivatives

FU Ben; TIAN Yuntao; DING Li; WU Qiuye; GUO Zhongwu; ZHAO Qingjie

doi:10.3969/j.issn.1006-0111.2017.01.004

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Objective To synthesize a series of 13-acylmatrine derivatives and evaluate their in vitro antitumor activity. Methods Using sophocarpine as the starting material,a series of new compounds were synthesized through Michael addition,Staudinger reduction and acylation.The structure of target compounds were confirmed by ¹H NMR and MS techniques. Their antitumor activity against human hepatoma cells(BEL-7404) and mice melanoma cells (K111) were evaluated in vitro by MTT assay. Results We synthesized 9 compounds and all the compounds exhibited inhibitory activities against BEL-7404 and K111. Conclusion Compound 4b and compound 4e exhibit good in vitro antitumor activity to human hepatoma cells (BEL-7404).

Synthesis and antitumor activity of 13-acylmatrine derivatives

Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

Received Date: 2016-07-27

Rev Recd Date: 2016-11-25

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Abstract: Objective To synthesize a series of 13-acylmatrine derivatives and evaluate their in vitro antitumor activity. Methods Using sophocarpine as the starting material,a series of new compounds were synthesized through Michael addition,Staudinger reduction and acylation.The structure of target compounds were confirmed by ¹H NMR and MS techniques. Their antitumor activity against human hepatoma cells(BEL-7404) and mice melanoma cells (K111) were evaluated in vitro by MTT assay. Results We synthesized 9 compounds and all the compounds exhibited inhibitory activities against BEL-7404 and K111. Conclusion Compound 4b and compound 4e exhibit good in vitro antitumor activity to human hepatoma cells (BEL-7404).

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Synthesis and antitumor activity of 13-acylmatrine derivatives

doi: 10.3969/j.issn.1006-0111.2017.01.004

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