High yield conversion of doxorubicin to 2-pyrrolinodoxorubicin, an analog 500-1000 times more potent: Structure-activity relationship of daunosamine-modified derivatives of doxorubicin

Attila Nagy; Patricia Armatis; Andrew V. Schally

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High yield conversion of doxorubicin to 2-pyrrolinodoxorubicin, an analog 500-1000 times more potent: Structure-activity relationship of daunosamine-modified derivatives of doxorubicin

机译：将阿霉素高产率转化为2-吡咯啉阿霉素，其效力高500-1000倍：柔红霉素经柔红霉素修饰的衍生物的结构活性关系

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摘要

A convenient, high yield conversion of doxo- rubicin to 3'-deamino-3'-(2"-pyrroline-1"-yl)doxorubicin is described. This daunosamine-modified analog of doxorubicin is 500-1000 times more active in vitro than doxorubicin. The conversion is effected by using a 30-fold excess of 4-iodobu- tyraldehyde in anhydrous dimethylformamide. The yield is higher than 85/100. A homolog of this compound, 3'-deamino- 3'-(1",3"-tetrahydropyridine-1"-yl)doxorubicin, was also syn- thesized by using 5-iodovaleraldehyde.

机译：描述了将阿霉素-红霉素方便，高产率地转化为3'-脱氨基-3'-（2“-吡咯啉-1”-基）多柔比星的方法。这种柔红霉素经柔红霉素修饰的类似物在体外的活性是阿霉素的500-1000倍。通过在无水二甲基甲酰胺中使用30倍过量的4-碘丁醛进行转化。产率高于85/100。该化合物的同系物3'-脱氨基-3'-（1“，3”-四氢吡啶-1“-基）多柔比星也通过使用5-碘戊醛合成。

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《Proceedings of the National Academy of Sciences of the United States of America》 |1996年第6期|p.2464-2469|共6页
作者
Attila Nagy; Patricia Armatis; Andrew V. Schally;
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收录信息美国《科学引文索引》(SCI);美国《生物学医学文摘》(MEDLINE);美国《化学文摘》(CA);
原文格式 PDF
正文语种 eng
中图分类自然科学总论;
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专利

1. Cytotoxic analogs of luteinizing hormone-releasing hormone containing doxorubicin or 2-pyrrolinodoxorubicin, a derivative 500-1000 times more potent [J] . Attila Nagy, Andrew V. Schally, Patricia Armatis Proceedings of the National Academy of Sciences of the United States of America . 1996,第14期

机译：含有阿霉素或2-吡咯啉阿霉素的促黄体激素释放激素的细胞毒性类似物，其衍生物的效价高500-1000倍
2. DNA interactions of 2-pyrrolinodoxorubicin, a distinctively more potent daunosamine-modified analogue of doxorubicin. [J] . Stepankova J, Studenovsky M, Malina J, Biochemical Pharmacology . 2011,第3期

机译：2-吡咯啉阿霉素的DNA相互作用，阿霉素是一种明显更有效的柔红霉素修饰的类似物。
3. Design, synthesis, and in vitro evaluation of cytotoxic analogs of bombesin-like peptides containing doxorubicin or its intensely potent derivative, 2-pyrrolinodoxorubicin [J] . Attila Nagy, Patricia Armatis, Ren-Zhi Cai Proceedings of the National Academy of Sciences of the United States of America . 1997,第2期

机译：设计，合成和体外评估含有阿霉素或其强效衍生物2-吡咯啉阿霉素的类蛙心素肽的细胞毒性类似物
4. Synergistic Cytotoxicity Effect by Combination Treatment of Polyketide Derivatives from Annona muricata Linn Leaves and Doxorubicin as Potential Anticancer Material on Raji Cell Line [C] . A N Artanti, O P Astirin, A Prayito International Conference on Advanced Materials for Better Future . 2018

机译：通过从Annona Muricata Linn叶片和多柔比星的聚酮衍生物组合治疗的协同细胞毒性效应作为Raji细胞系的潜在抗癌材料
5. Design, synthesis, and evaluation of potent androgen receptor targeted prodrugs of doxorubicin. [D] . Cogan, Peter Smith. 2003

机译：设计，合成和评估有效的雄激素受体靶向的阿霉素前药。
6. High yield conversion of doxorubicin to 2-pyrrolinodoxorubicin an analog 500-1000 times more potent: structure-activity relationship of daunosamine-modified derivatives of doxorubicin. [O] . A Nagy, P Armatis, A V Schally 1996

机译：阿霉素到2-吡咯啉阿霉素的高产率转化类似物的效价比阿霉素修饰的阿霉素衍生物强500-1000倍。
7. High yield conversion of doxorubicin to 2-pyrrolinodoxorubicin, an analog 500-1000 times more potent: structure-activity relationship of daunosamine-modified derivatives of doxorubicin. [O] . Nagy, A, Armatis, P, Schally, A V 1996

机译：阿霉素到2-吡咯啉阿霉素的高产率转化，类似物的效价比阿霉素修饰的阿霉素衍生物强500-1000倍。

High yield conversion of doxorubicin to 2-pyrrolinodoxorubicin, an analog 500-1000 times more potent: Structure-activity relationship of daunosamine-modified derivatives of doxorubicin

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