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稠合喹啉衍生物的合成与抗肿瘤活性。III. 新型N-糖基氨基-吲哚并[3,2-b]喹啉

Synthesis and antitumor activity of fused quinoline derivatives. III. Novel N-glycosylamino-indolo[3,2-b]quinolines.

作者信息

Takeuchi Y, Chang M R, Hashigaki K, Tashiro T, Tsuruo T, Tsukagoshi S, Yamato M

机构信息

Faculty of Pharmaceutical Sciences, Okayama University, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1992 Jun;40(6):1481-5. doi: 10.1248/cpb.40.1481.

DOI:10.1248/cpb.40.1481
PMID:1394666
Abstract

Novel indolo[3,2-b]quinolines (1b-k), having a nitro, amino, acetamido, methanesulfonamido, or glycosylamino group at the 2, 7, or 8-position, were prepared and their antitumor activities against P388 leukemia in mice were examined. The 7-galactopyranosylamino derivative (1g) showed the most potent activity (optimal dose = 25 mg/kg, T/C greater than 333%, cure rate 5/6).

摘要

制备了在2、7或8位带有硝基、氨基、乙酰氨基、甲磺酰胺基或糖基氨基的新型吲哚并[3,2 - b]喹啉(1b - k),并检测了它们对小鼠P388白血病的抗肿瘤活性。7 - 吡喃半乳糖基氨基衍生物(1g)表现出最强的活性(最佳剂量 = 25 mg/kg,T/C大于333%,治愈率5/6)。

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