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有机化学
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有机化学 ›› 2007, Vol. 27 ›› Issue (05): 629-635. 上一篇    下一篇

研究论文

N-4-羟基苯基维甲酰胺与呋咱氮氧化物偶联物的合成及抗肿瘤活性研究

郝北辰a，张奕华*,a，赖宜生a，袁胜涛b，张陆勇b   

  1. (a中国药科大学新药研究中心 南京 210009)
    (b中国药科大学新药筛选中心 南京 210009)
  • 收稿日期:2006-08-10 修回日期:2006-09-23 发布日期:2007-05-10
  • 通讯作者: 张奕华

Studies on Synthesis and Anti-tumor Activity of Conjugates ofFuroxans to N-(4-Hydroxyphenyl)retinamide

HAO Bei-Chena, ZHANG Yi-Hua*,a, LAI Yi-Shenga, YUAN Sheng-Taob
ZHANG Lu-Yongb   

  1. (a Center of New Drug Research, China Pharmaceutical University, Nanjing 210009)
    (b Center of Drug Screening, China Pharmaceutical University, Nanjing 210009)
  • Received:2006-08-10 Revised:2006-09-23 Published:2007-05-10
  • Contact: ZHANG Yi-Hua

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为了寻找治疗乳腺癌的药物, 将N-4-羟基苯基维甲酰胺(4-HPR)以乙酸为连接基团通过酯键或酰胺键与NO供体呋咱氮氧化物缀合, 合成了NO供体型维甲酸类化合物, 共11个新的目标化合物, 其结构经IR, MS, 1H NMR和元素分析表征, 总收率为8.8%～12.9%. 对目标物进行体外抗乳腺癌活性测试, 结果表明, 所有目标物均具有不同程度的抗肿瘤活性, 其中8g抗肿瘤活性和对照药阿霉素相当.

关键词: 一氧化氮供体, 维甲酸类化合物, 抗肿瘤活性, 合成

To search for potential anti-breast cancer drugs, coupling N-(4-hydroxyphenyl)retinamide (4-HPR) with NO donor furoxans through esterification or amidation, a series of NO-donating retinoids were designed and synthesized, and their structures were established by MS, IR, 1H NMR spectra and elemental analysis. The total yield was 8.8%～12.9%. The anti-breast cancer activities of these target compounds were tested in vitro. Preliminary biological activity test indicated that all target compounds showed anti-tumor effects to a certain degree, among which compound 8g was as potent as anti-tumor drug adriamycin.

Key words: NO donor, retinoid, anti-tumor activity, synthesis