4-Demethoxy-3 -N-trifluoroacetyldoxorubicin。合成及实体瘤活性。

Drug design and delivery Pub Date : 1990-06-01

D Horton, W Priebe, J P Carter, J Filppi, R L Wolgemuth

{"title":"4-Demethoxy-3 -N-trifluoroacetyldoxorubicin。合成及实体瘤活性。","authors":"D Horton, W Priebe, J P Carter, J Filppi, R L Wolgemuth","doi":"","DOIUrl":null,"url":null,"abstract":"A new route has been developed for the preparation of 3'-N-protected doxorubicin analogues. 4-Demethoxy-3'-N-trifluoroacetyldoxorubicin (5) was synthesized in an approach to an orally active anthracycline analogue. Tested against the B-16 murine solid tumor in mice, this compound increased life span by 133% when it was administered intraperitoneally at 25 mg/kg, and by 52% when it was given orally at 50 mg/kg.","PeriodicalId":11271,"journal":{"name":"Drug design and delivery","volume":"6 2","pages":"123-9"},"PeriodicalIF":0.0000,"publicationDate":"1990-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"4-Demethoxy-3'-N-trifluoroacetyldoxorubicin. Synthesis and solid tumor activity.\",\"authors\":\"D Horton, W Priebe, J P Carter, J Filppi, R L Wolgemuth\",\"doi\":\"\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"A new route has been developed for the preparation of 3'-N-protected doxorubicin analogues. 4-Demethoxy-3'-N-trifluoroacetyldoxorubicin (5) was synthesized in an approach to an orally active anthracycline analogue. Tested against the B-16 murine solid tumor in mice, this compound increased life span by 133% when it was administered intraperitoneally at 25 mg/kg, and by 52% when it was given orally at 50 mg/kg.\",\"PeriodicalId\":11271,\"journal\":{\"name\":\"Drug design and delivery\",\"volume\":\"6 2\",\"pages\":\"123-9\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1990-06-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Drug design and delivery\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drug design and delivery","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}

引用次数: 0

摘要

为制备3′- n保护的阿霉素类似物开辟了一条新途径。4-去甲氧基-3'- n -三氟乙酰多柔比星(5)以一种口服活性蒽环类类似物的方法合成。对小鼠B-16实体瘤进行的实验表明，以25 mg/kg腹腔给药可延长133%的寿命，以50 mg/kg口服可延长52%的寿命。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

微信好友朋友圈 QQ好友复制链接

本刊更多论文

4-Demethoxy-3'-N-trifluoroacetyldoxorubicin. Synthesis and solid tumor activity.

A new route has been developed for the preparation of 3'-N-protected doxorubicin analogues. 4-Demethoxy-3'-N-trifluoroacetyldoxorubicin (5) was synthesized in an approach to an orally active anthracycline analogue. Tested against the B-16 murine solid tumor in mice, this compound increased life span by 133% when it was administered intraperitoneally at 25 mg/kg, and by 52% when it was given orally at 50 mg/kg.

求助全文

通过发布文献求助，成功后即可免费获取论文全文。去求助

来源期刊

Drug design and delivery

自引率

0.00%

发文量