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- [1] METABOLISM AND ACTION OF AMINO-ACID ANALOG ANTICANCER AGENTS[J]. PHARMACOLOGY & THERAPEUTICS, 1990, 46 (02) : 243 - 271AHLUWALIA, GSGREM, JLHAO, ZCOONEY, DA
- [3] ZHAO M, 1999, J PRAKT CHEM, V341, pR30
Synthesis of 6-amino acid substituted 4,6,7,12-tetrahydro-4-oxoindolo[2, 3-a]quinolizines
被引：0
作者：
Zhao, M
Wang, C
Guo, M
Peng, SQ
[1
]
Winterfeldt, E
机构：
[1] Beijing Med Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China
[2] Univ Hannover, Inst Organ Chem, D-3000 Hannover, Germany
来源：
JOURNAL FUR PRAKTISCHE CHEMIE-CHEMIKER-ZEITUNG
|
1999年
/
341卷
/
07期
关键词：
antitumor agents;
nitrogen heterocycles;
synthesis design;
indoloquinolizes;
quinolizines;
D O I：
10.1002/(SICI)1521-3897(199910)341:7<691::AID-PRAC691>3.3.CO;2-O
中图分类号：
O69 [应用化学];
学科分类号：
081704 ;
摘要：
In the presence of Na2CO3 (1S, 3S)- and (1R, 3S)-1-(2,2-dimethoxyethyl)-2-(1,3-dioxobutyl)-3-(1,3-dioxobutyl)oxymethyl-1,2,3,4-tetrahydrocarboline (1) were transformed into (1S, 3S)- and (1R, 3S)-1-(2,2-dimethoxyethyl)-2-(1,3-dioxobutyl)-3-hydroxymethyl-1,2,3,4-tetrahydrocarboline (2) which were cyclized to (6S)-3-acetyl-6-hydroxymethyl-4,6,7,12-tetrahydro-4-oxoindolo[2, 3-a]quinolizine (4), via (6S, 12bS)- and (6S, 12bR)-3-acetyl-2-hydroxyl-6-hydroxymethyl-1,2,3,4,6,7,12,1 2b-octahydro-4-oxoindolo[2,3-a] quinoline (3). (6S)-4 was coupled with Boc-Gly, Boc-L-Asp (beta-benzyl ester), or Boc-L-Gln to give 6-amino acid substituted (6S)-3-acetyl-4,6,7,12-tetrahydro-4-oxoindolo[2,3-a]quinolizines 5a, 5b, or 5c, respectively. After the removal of Boc from (6S)-5a (6S)-3-acetyl-6-glycyl-4,6,7,12-tetrahydro-4-oxoindolo[2,3-a]quinolizine (6) was obtained. The anticancer activities of (6S)-5 and (6S)-6 in vitro were tested.
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页码：691 / 694
页数：4
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