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7-(N-糖基氨基)-吲哚并[3,2-b]喹啉的合成及其抗肿瘤活性

Synthesis and antitumor activity of 7-(N-glycosylamino)-indolo[3,2-b]quinolines.

作者信息

Takeuchi Y, Chang M R, Hashigaki K, Yamato M

机构信息

Faculty of Pharmaceutical Sciences, Okayama University, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1991 Jun;39(6):1629-31. doi: 10.1248/cpb.39.1629.

Abstract

Novel indolo[3,2-b]quinolines (1d-g), introduced at the 7-position with an N-glycosylamino group, were prepared and their antitumor activities against leukemia P388 in mice were examined. The N-Galactopyranosylamino derivative (1e) was a much more potent anti-leukemia compound (optimal dose = 25 mg/kg, T/C greater than 333%, cure 5/6) than lead compound 1a.

摘要

制备了在7位引入N-糖基氨基的新型吲哚并[3,2-b]喹啉(1d-g),并检测了它们对小鼠白血病P388的抗肿瘤活性。N-吡喃半乳糖基氨基衍生物(1e)是一种比先导化合物1a更有效的抗白血病化合物(最佳剂量=25mg/kg,T/C大于333%,治愈5/6)。

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