高等学校化学学报

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α-氨基酸的新型有机锗化合物的合成与生物活性研究

陈建新1, 陈莉1, 翟玉平2, 史寅2, 孙丽娟1   

    1. 南开大学元素有机化学重点实验室,
    2. 化学学院化学系, 天津 300071
  • 收稿日期:2005-06-27 修回日期:1900-01-01 出版日期:2006-08-10 发布日期:2006-08-10
  • 通讯作者: 孙丽娟

Syntheses of Novel Organogermanium Compounds Containing α-Amino Acid and Studies on the Antitumor Activity

CHEN Jian-Xin1, CHEN Li1, ZHAI Yu-Ping2, SHI Yin2, SUN Li-Juan1   

    1. State Key Laboratory of Elemento-Organic Chemistry,
    2. Department of Chemistry, College of Chemistry, Nankai University, Tianjin 300071, China
  • Received:2005-06-27 Revised:1900-01-01 Online:2006-08-10 Published:2006-08-10
  • Contact: SUN Li-Juan

摘要: 设计合成了两个系列20个含α-氨基酸的新型有机锗化合物, 对化合物进行了波谱表征, 用X射线衍射测定了化合物Ph3GeCH(Ph)CH2CONHCH(CH2COOC2H5)COOC2H5的晶体结构. 抗肿瘤实验结果表明, 这两个系列的化合物有一定的抗KB, HCT-8和Bel-7402活性.

关键词: 有机锗化合物, α-氨基酸, 晶体结构, 抗肿瘤活性

Abstract: In order to search new organogermanium antitumor drugs with an activity and low toxicity, 20 new organogermanium compounds were designed and synthesized by attaching α-amino acid to organogermanium moieties. Their structures were confirmed by IR, 1H NMR and elemental analysis. The crystal structure of Ph3GeCH(Ph)CH2CONHCH(CH2COOC2H5)COOC2H5 were determined by X-ray diffraction. Three human neoplastic cell lines(KB, HCT-8 and Bel-7402) were used to screen these compounds. The results indicate that some compounds at 5 μmol/L show a weak in vitro antitumor activity.

Key words: Organogermanium compound, α-Amino acid, Crystal structure, Antitumor activity

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