| NO供体型硝酸酯类甘草次酸衍生物的合成及抗肿瘤活性 |
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| 引用本文： | 申利红,张奕华,赖宜生,罗旭馨,袁胜涛,张陆勇.NO供体型硝酸酯类甘草次酸衍生物的合成及抗肿瘤活性[J].中国药科大学学报,2011,42(1):34-38. |
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| 作者姓名： | 申利红 张奕华 赖宜生 罗旭馨 袁胜涛 张陆勇 |
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| 作者单位： | 中国药科大学新药研究中心;邯郸学院化学系;中国药科大学新药筛选中心; |
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| 摘 要： | 甘草次酸的3位羟基和30位羧基通过脂肪链连接基团引入硝酸酯结构片段,合成了9个新的NO供体型硝酸酯类甘草次酸衍生物(4a～4f,8a～8c)。目标化合物的结构均经红外光谱、质谱、磁共振氢谱确证。体外采用MTT法测定了目标化合物对4种人肿瘤细胞株增殖的抑制活性,结果表明部分目标化合物对人肝癌细胞(HepG2和BEL-7402)、人乳腺癌细胞MCF-7和人早幼粒细胞白血病细胞HL-60的增殖具有较好的抑制活性。
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| 关 键 词： | 甘草次酸 NO供体 硝酸酯 合成 抗肿瘤活性 |
Synthesis and antitumor activity of nitric oxide-donating glycyrrhetinic acid derivatives coupled with nitrate moiety |
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| SHEN Li-hong,ZHANG Yi-hu,LAI Yi-sheng,LUO Xu-xin,YUAN Sheng-tao and ZHANG Lu-yong.Synthesis and antitumor activity of nitric oxide-donating glycyrrhetinic acid derivatives coupled with nitrate moiety[J].Journal of China Pharmaceutical University,2011,42(1):34-38. |
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| Authors: | SHEN Li-hong ZHANG Yi-hu LAI Yi-sheng LUO Xu-xin YUAN Sheng-tao and ZHANG Lu-yong |
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| Institution: | SHEN Li-hong1,2,ZHANG Yi-hua1,LAI Yi-sheng1,LUO Xu-xin3,YUAN Sheng-tao3,ZHANG Lu-yong3 1Center of Drug Discovery,China Pharmaceutical University,Nanjing 210009,2Department of Chemistry,Handan College,Handan 056005,3Center of Drug Screening,China |
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| Abstract: | Nine new nitric oxide-donating derivatives of glycyrrhetinic acid coupled with nitrate moieties were designed,synthesized,and evaluated for their in vitro cytotoxicity against four cancer cell lines by MTT assay.Nitrate moieties were conjugated with C3-OH or/and C30-COOH of glycyrrhetinic acid via a variety of aliphatic linkers,affording the target compounds 4a-4f and 8a-8c,respectively,and their structures were confirmed by MS,IR and 1H NMR.The MTT assay demonstrated that some of the target compounds exhib... |
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| Keywords: | glycyrrhetinic acid NO donor nitrate synthesis antitumor activity |
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