Modification of the antibiotic olivomycin I at the 2'-keto group of the side chain. Novel derivatives, antitumor and topoisomerase I-poisoning activity.

Tevyashova AN; Olsufyeva EN; Balzarini J; Shtil AA; Dezhenkova LG; Bukhman VM; Zbarsky VB; Preobrazhenskaya MN

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Modification of the antibiotic olivomycin I at the 2'-keto group of the side chain. Novel derivatives, antitumor and topoisomerase I-poisoning activity.

机译：在侧链的2'-酮基上修饰抗生素寡霉素I。新型衍生物，抗肿瘤和拓扑异构酶I中毒活性。

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A novel way of chemical modification of the antibiotic olivomycin I at the 2'-keto group of the side chain of the aglycone moiety was developed. Reaction of olivomycin I with the carboxymethoxylamine hemihydrochloride gave the key intermediate, 2'-carboxymethoxime-olivomycin I, which was further reacted with different amines in the presence of benzotriazol-1-yl-oxy-trispyrrolidinophosphonium hexafluorophosphate to give the corresponding amides. The antiproliferative and topoisomerase I (Topo-I)-poisoning activities of the novel derivatives were examined. One of the novel derivatives showed a marked inhibitory activity against Topo-I, a pronounced antitumor activity in in vivo experiments on mice bearing leukemia P-388 and lower toxic side effects compared with the parent olivomycin I.

机译：开发了在糖苷配基部分的侧链的2'-酮基上化学修饰抗生素寡霉素I的新方法。橄榄霉素I与羧甲氧基胺半盐酸盐的反应生成了关键中间体2'-羧甲基肟-橄榄霉素I，该中间体在六氟磷酸苯并三唑-1-基-氧基-三吡咯烷基磷鎓的存在下与不同的胺进一步反应，得到相应的酰胺。研究了新型衍生物的抗增殖和拓扑异构酶I（Topo-I）中毒活性。一种新的衍生物显示出对Topo-I的显着抑制活性，在体内实验中对患有白血病P-388的小鼠具有明显的抗肿瘤活性，并且与亲本寡霉素I相比，毒性副作用更低。

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《The Journal of Antibiotics: An International Journal》 |2009年第1期|共5页
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Tevyashova AN; Olsufyeva EN; Balzarini J; Shtil AA; Dezhenkova LG; Bukhman VM; Zbarsky VB; Preobrazhenskaya MN;
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1. Modification of the antibiotic olivomycin I at the 2'-keto group of the side chain. Novel derivatives, antitumor and topoisomerase I-poisoning activity. [J] . Tevyashova AN, Olsufyeva EN, Balzarini J, The Journal of Antibiotics: An International Journal . 2009,第1期

机译：在侧链的2'-酮基上修饰抗生素寡霉素I。新型衍生物，抗肿瘤和拓扑异构酶I中毒活性。
2. Modification of the antibiotic olivomycin I at the 2'-keto group of the side chain. Novel derivatives, antitumor and topoisomerase I-poisoning activity. [J] . Tevyashova AN, Olsufyeva EN, Balzarini J, The Journal of Antibiotics: An International Journal . 2009,第1期

机译：在侧链的2'-酮基团中修饰抗生素寡霉素I。新型衍生物，抗肿瘤和拓扑异构酶I-中毒活性。
3. Modification of the antibiotic olivomycin I at the 2'-keto group of the side chain. Novel derivatives, antitumor and topoisomerase I-poisoning activity. [J] . Tevyashova AN, Olsufyeva EN, Balzarini J, The Journal of Antibiotics: An International Journal . 2009,第1期

机译：在侧链的2'-酮基团中修饰抗生素寡霉素I。新型衍生物，抗肿瘤和拓扑异构酶I-中毒活性。
4. Specific inhibition of human DNA ligase adenylation by a distamycin derivative possessing antitumor activity. [O] . A Montecucco, M Fontana, F Focher, 1991

机译：具有抗肿瘤活性的双霉素衍生物对人DNA连接酶腺苷酸的特异性抑制。
5. UCE6, a New Antitumor Antibiotic with Topoisomerase I-mediated DNA Cleavage Activity Produced by Actinomycetes: Producing Organism,Fermentation, Isolation and Biological Activity. [O] . NOBORU FUJII, FUTOSHI TANAKA, YOSHINORI YAMASHITA, 1997

机译：UCE6，一种新的抗肿瘤抗生素，具有拓扑异构酶I介导的DNA切割活性，由放线菌产生：产生生物，发酵，分离和生物活性。

Modification of the antibiotic olivomycin I at the 2'-keto group of the side chain. Novel derivatives, antitumor and topoisomerase I-poisoning activity.

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