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2—(1—羟基)乙基二氢卟吩f及其醚衍生物的合成和肿瘤光生物活性
引用本文:姚建忠,刘建飞,张万年,章玲,周有骏,吕加国,朱驹,王小燕.2—(1—羟基)乙基二氢卟吩f及其醚衍生物的合成和肿瘤光生物活性[J].中国药物化学杂志,2001,11(1):1-4.
作者姓名:姚建忠  刘建飞  张万年  章玲  周有骏  吕加国  朱驹  王小燕
作者单位:第二军医大学药学院,上海 200433
基金项目:国家自然科学基金资助项目(39522003)
摘    要:以蚕沙叶绿素稳定降解产物二氢卟吩f(2)为关键中间体,设计合成了2-(1-羟基)乙基二氢卟吩f(3a)3及其醚类衍生物3b-3d、4b-4d,其中,3a.4c.4d为新化合物,用UV.IR.^1HNMR和FAB-MS确证了它们的结构。同时测定了目标物3a.4b-4d对小鼠肉瘤-180移植瘤的光动力治疗作用,结果显示:2-(1-羟基)乙基二氢卟吩f醚衍生物4b-4d对小鼠肉瘤-180移植瘤的光动力治疗效果均优于参比药物血卟啉生物(HpD),且随醚链增长而增强,而3a却无效,这将对进一步的构效关系研究具有重要的意义。

关 键 词:蚕沙  叶绿素  2-(1-羟基)乙基二氢卟吩f  醚衍生物  合成  肿瘤  光动光动力治疗
文章编号:1005-0108(2001)01-0001-04
修稿时间:2000年8月28日

Synthesis and Tumor-Photobiological Activities of 2-(1-Hydroxyl)ethyl chlorin f and Its Ether Derivatives
YAO Jian zhong,LIU Jian fei,ZHANG Wan nian,ZHANG Ling,ZHOU You jun,LU Jia guo,ZHU Ju,WANG Xiao yan.Synthesis and Tumor-Photobiological Activities of 2-(1-Hydroxyl)ethyl chlorin f and Its Ether Derivatives[J].Chinese Journal of Medicinal Chemistry,2001,11(1):1-4.
Authors:YAO Jian zhong  LIU Jian fei  ZHANG Wan nian  ZHANG Ling  ZHOU You jun  LU Jia guo  ZHU Ju  WANG Xiao yan
Abstract:2-(1-hydroxyl)ethyl chlorin f(3a)and its six etherderivatives(3b~3d、4b~4d)were designed and synthesized via HBr addition of 2-vinyl of chlorin f(2)which was prepared through acidic and alkaline oxidative degradation using silkworm excrement crude chlorophyll extracts as the starting material followed by H2O,MeOH,n-C3H7OH,n-C5H11 nucleophilic substitution and hydrolysis.3a,3c,3d,4c and 4d were new compounds.Their structures were confirmed by UV,IR,1H-NMR and FAB-MS.The photodynamic effects of the target compounds(3a,4b,4c and 4d)on sarcoma 180 transplanted in mice were determined.The results of preliminary experiment showed that 4b,4c and 4d had more efficacious photochemotherapeutic potency than that of HpD,and 4d was the best among them,but 3a had no photochemotherapeutic potency.It is suggested that the photochemotherapeutic potency of 2-(1-hydroxyl)ethyl chlorin f ether derivatives on sarcoma 180 transplanted in mice enhance as their chain length increase and further studies on their structure-action-relationship(SAR)seem to be of importance as well.
Keywords:silkworm excrement  chlorophyll  2  (1  hydroxyl)ethyl chlorin f  ether derivatives  synthesis  neoplasm  photodynamic therapy
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