synthesis and cytotoxicity evaluation of 13-n-alkyl berberine and palmatine analogues as anticancer agents合成和细胞毒性评价13-n-alkyl小檗碱和非洲防己碱类似物作为抗癌药物.pdf

Molecules 2012, 17, 11294-11302; doi:10.3390/molecules171011294 OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis and Cytotoxicity Evaluation of 13-n-Alkyl Berberine and Palmatine Analogues as Anticancer Agents Lei Zhang 1, Jingjing Li 1, Fei Ma 2,3, Shining Yao 4, Naisan Li 1, Jing Wang 1, Yongbin Wang 1, Xiuzhen Wang 5 and Qizheng Yao 1,* 1 School of Pharmacy, China Pharmaceutical University, Nanjing 210009, Jiangsu, China; E-Mails: zhanglei04402@163.com (L.Z.); leejingjing119@ (J.L.); linaisan@ (N.L.); wangjing0642320@126.com (J.W.); wybhzsyq@126.com (Y.W.) 2 Oil Crops Research Institute, Chinese Academy of Agricultural Sciences, Wuhan 430062, Hubei, China; E-Mail: mafeicpu@163.com 3 Key Laboratory of Biology and Genetic Improvement of Oil Crops, Ministry of Agriculture, Wuhan 430062, Hubei, China 4 Wuxi JC Pharmaceutical Technology Inc., Wuxi 214036, Jiangsu, China; E-Mail: yao_sn@ 5 School of Pharmacy, Nanjing Medical University, Nanjing 210029, Jiangsu, China; E-Mail: showshow828@163.com * Author to whom correspondence should be addressed; E-Mail: qz_yao@; Tel./Fax: +86-025-8663-4730. Received: 30 August 2012; in revised form: 11 September 2012 / Accepted: 17 September 2012 / Published: 25 September 2012 Abstract: By introducing long carbon-chain alkyl groups at the C-13 position of berberine and palmatine, 13-n-hexyl/13-n-octyl berberine and palmatine chloride analogues 4a–d were synthesized and examined by MTT assays for cytotoxic activity in seven human cancer cell lines