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抗癌新药埃博霉素的研究与开发(一) 被引量:4

R & D of a New Anti-cancer Drug:Epothilone
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摘要 埃博霉素(也称埃坡霉素、埃坡西龙,英文:epothilones)是由黏细菌纤维素堆囊菌分泌的结构为16元内酯大环为中心体、噻唑环配基为侧链的一类细胞毒性化合物,是一种具有类似紫杉醇微管蛋白聚合和微管稳定作用的新抗肿瘤药物,埃博霉素类似物结构式见图1。 Epothilone is one kind of natural product with characters of stabilizing microtubule as paclitaxel (Taxol).Among stabilizing microtubular products,the lactam analogues of the epothilone B and some of its derivatives have emerged as particularly promising candidates for commercial development.The total and semi-synthesis technologies of these compounds were described in this article.At the same time,the semisynthesis of epothilone D was introduced emphatically,and the recent progresses in research of the biological activity were discussed.
出处 《精细与专用化学品》 CAS 2008年第5期17-19,共3页 Fine and Specialty Chemicals
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  • 1沈清清.粘细菌的生态作用探究[J].科技资讯,2008,6(13). 被引量:1
  • 2唐慧,刘新利,李越中.纤维堆囊菌子实体提取物的急性毒性和遗传毒性分析[J].预防医学论坛,2005,11(2):193-195. 被引量:2
  • 3李玉美,高俊,杨志杰,林明丽.大孔树脂吸附和分离牛心朴子草中生物碱的研究[J].内蒙古工业大学学报(自然科学版),2007,26(1):38-41. 被引量:11
  • 4刘新利,李越中.粘细菌次级代谢产物及其在农业上的应用价值[J].中国农业科技导报,2007,9(3):44-51. 被引量:12
  • 5Hofle G H, Bedorf H, Steinmetz H, et al. Epothilone A and B-Novel 16-Membered Macrolides with Cytotoxic Activity: Isolation, Crystal Structure, and Conformation in Solution [J]. AngewChem Int Ed Engl, 1996,35:1567.
  • 6Girth K, Bedorf N, HOfle G, etal. Epothilone A and B: Antifungal and Cytotoxic Compounds from Sorangium cellulosum (Myxobacteria) Production, Physico-chemical and Biological Properities[J]. J Antibiol, 1996,49: 560.
  • 7Hofle G, Glaser N, Leibold T, etal. Semisynthesis and deg radation of the tubulin inhibitors epothilone and tubulysin [J]. Pure Appl Chem, 2003,75.. 167.
  • 8Su DS, Ballog A, Meng D. Total synthesis of epothilone B: An extension of the Suzuki coupling method and insights into structure-activity relationships of the Epothilones[J]. Angezv Chem Int Ed, 1997,36:757.
  • 9Meng D, Kamenecka T, Danishefsky S, et al. Second generation epothilones: discovery of fludelone and its extraordinary antitumor properties[J]. Ange'w Chem Int Ed , 1996,35: 2801.
  • 10Schinzer D, Limberg A, Bauer A, et al. Total Synthesis of (-)-Epothilone A[J]. Angevo Chem Int Ed , 1997,:36: 523.

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