| 新型蜀羊泉碱衍生物的合成及体外抗肿瘤活性 |
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| 引用本文： | 查晓明,张斐然,单佳祺,陈艳客,张奕华,刘 钧,孙宏斌.新型蜀羊泉碱衍生物的合成及体外抗肿瘤活性[J].中国药科大学学报,2010,41(6):493-498. |
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| 作者姓名： | 查晓明 张斐然 单佳祺 陈艳客 张奕华 刘 钧 孙宏斌 |
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| 作者单位： | 中国药科大学新药研究中心,中国药科大学新药筛选中心;约翰·霍普金斯大学医学院;中国药科大学新药研究中心;中国药科大学新药研究中心;中国药科大学新药研究中心;约翰·霍普金斯大学医学院;中国药科大学新药研究中心 |
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| 摘 要： | 蜀羊泉碱是一类来源于白英的甾体生物碱，具有多种生物活性。本文通过对其C-3位羟基、E环和F环进行结构修饰，合成了10个蜀羊泉碱衍生物，并对人前列腺癌细胞PC-3进行了体外癌细胞增殖抑制实验。体外实验显示部分化合物对人前列腺癌细胞PC-3有较好增殖抑制作用，其中化合物 19 活性最好，其IC 50为（4.8±0.9）μmol/L。
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| 关 键 词： | 蜀羊泉碱衍生物 合成 抗肿瘤活性 |
Synthesis and in vitro antitumor activities of novel soladulcidine derivatives |
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| ZHA Xiao-ming,ZHANG Fei-ran,SHAN Jia-qi,CHEN Yan-ke,ZHANG Yi-hu,LIU Jun and SUN Hong-bin.Synthesis and in vitro antitumor activities of novel soladulcidine derivatives[J].Journal of China Pharmaceutical University,2010,41(6):493-498. |
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| Authors: | ZHA Xiao-ming ZHANG Fei-ran SHAN Jia-qi CHEN Yan-ke ZHANG Yi-hu LIU Jun and SUN Hong-bin |
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| Institution: | ZHA Xiao-ming1,2,ZHANG Fei-ran3,SHAN Jia-qi1,CHEN Yan-ke1,ZHANG Yi-hua1,LIU Jun3,SUN Hong-bin1 1Center for Drug Discovery,2Jiangsu Provincial Center for Drug Screening,China Pharmaceutical University,Nanjing 210009,China,3Department of Pharmacology and Oncology,Johns Hopkins University School of Medicine,Baltimore,MD 21205,USA |
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| Abstract: | Soladulcidine is a steroidal alkaloid abundant in Solanum dulcamara L.with antitumor and other biological activities.In this study,ten soladulcidine derivatives were synthesized through esterification at C-3-hydroxy group,modification at NH group of F ring or esterification of E ring-opening products.The in vitro antiproliferative activity of these synthesized derivatives against prostate cancer(PC-3) cell line was assessed.Within this series of compounds,compound 19 exhibited the most potent inhibitory eff... |
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| Keywords: | soladulcidine derivatives synthesis antitumor activity |
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