YAKHAK HOEJI (약학회지)
- Volume 40 Issue 2
- /
- Pages.117-125
- /
- 1996
- /
- 0377-9556(pISSN)
- /
- 2383-9457(eISSN)
Synthesis and Antitumor Activity of 3'-hydroxydaunorubicin and 3'-hydroxydoxorubicin Derivatives Substituted with 4'-fluorine or 4'-azide in Sugar Moiety
당부분에서 4'-플루오린 또는 4'-아자이드로 치환된 3'-히드록시다우노루비신과 3'-히드록시독소루비신 유도체의 합성과 항암활성
- Ok, Kwang-Dae (Research Laboratories, Dong-A Pharm. Co., Ltd.) ;
- Park, Jeong-Bae (Research Laboratories, Dong-A Pharm. Co., Ltd.) ;
- Kim, Moon-Sung (Research Laboratories, Dong-A Pharm. Co., Ltd.) ;
- Jung, Dong-Yoon (Research Laboratories, Dong-A Pharm. Co., Ltd.) ;
- Yang, Junn-Ick (Research Laboratories, Dong-A Pharm. Co., Ltd.)
- Published : 1996.04.01
Abstract
3'-Deamino-3-hydroxy-4'-fluoro- or 3'-deamino-3'-hydroxy-4'-azido-daunorubicin(6,8) and -doxorubicin(7,9) have been synthesized, respectively. Compounds 7,8 and 9 were mo re cytotoxic than daunorubicin(1) and doxorubicin(2) against L1210 murine leukemic cell in vitro. When administered intraperitoneally for 9 days starting 1 day after tumor inoculation, compounds 7(T/C 605%) and 9(T/C 488%) showed significant antitumor activity for ip-inoculuated L1210 murine leukemia at wide range of doses.