| 5-氟尿嘧啶短肽的合成及其抗肿瘤活性研究 |
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| 引用本文： | 卓仁禧,范昌烈,赵儒林.5-氟尿嘧啶短肽的合成及其抗肿瘤活性研究[J].有机化学,1986(2). |
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| 作者姓名： | 卓仁禧 范昌烈 赵儒林 |
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| 作者单位： | 武汉大学化学系 武汉 |
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| 摘 要： | 5-氟尿嘧啶乙酸对-硝基苯酯和5-氟尿嘧啶丙酸对-硝基苯酯分别与三种二肽反应,制备了五个5-氟尿嘧啶二肽(4 a-e)。以5-氟尿嘧啶的氨基酸对-硝基苯酯(2 a-c)分别和三种二肽反应,制得四个5-氟尿嘧啶三肽(5 a-d)。产物经元素分析、NMR、IR和UV鉴定。初步动物试验表明:5-氟尿嘧啶丙酰甘-苯丙二肽,5-氟尿嘧啶乙酰甘-甘-苯丙三肽和5-氟尿嘧啶乙酰缬-亮-甘三肽对小白鼠移植性艾氏腹水癌有一定的抑制作用。
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| 关 键 词： | 二肽 多肽 氟尿嘧啶 生物活性 抗癌药 制备 |
SYNTHESIS AND ANTITUMOR ACTIVITIES OF 5-FLUOROURACIL SMALL PEPTIDES |
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| Zhuo Renxi,Fan Changlie,Zhao Rulin.SYNTHESIS AND ANTITUMOR ACTIVITIES OF 5-FLUOROURACIL SMALL PEPTIDES[J].Chinese Journal of Organic Chemistry,1986(2). |
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| Authors: | Zhuo Renxi Fan Changlie Zhao Rulin |
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| Institution: | Zhuo Renxi,Fan Changlie,Zhao Rulin Department of Chemistry,Wuhan University,Wuhan |
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| Abstract: | 5-Fluorouracil(5-FU)dipeptides,5-FU-CH_2CO-Gly-Gly,5-FU-
CH_2CO-Gly-Phe,5-FU-CH_2CO-Gly-Leu,5-FU-CH_2CH_2CO-Gly-Gly and 5-FU-
CH_2CH_2CO-Gly-Phe were prepared by reacting 5-FU-CH_2COOC_6H_4NO_2 or 5-FU-
CH_2CH_2COOC_6H_4NO_2 with Gly-Gly,Gly-Phe and Gly-Leu.Also,by reaction of
5-FU-CH_2CO-GlyOC_6H_4NO_2,5-FU-CH_2CO-ValOC_6H_4NO_2 and 5-FU-CH_2CH_2CO-
PheOC_6H_4NO_2 with Gly-Phe,Leu-Gly and Ala-Gly,four 5-fluorouracil tripeptides
were prepared.The structures of these new peptides were characterized by ~1H NMR,
IR and UV spectra,as well as elemental analysis.The antitumor activities against
Ehrlich ascites carcinoma in mice were observed,the results being listed in Table 3. |
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| Keywords: | dipeptide polypcptide fluorouracil biological activity anticarcinogen preparation |
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