稠合喹啉衍生物的合成与抗肿瘤活性。V. 甲基吲哚并[3,2 - b]喹啉

Synthesis and antitumor activity of fused quinoline derivatives. V. Methylindolo[3,2-b]quinolines.

作者信息

Takeuchi Y, Kitaomo M, Chang M R, Shirasaka S, Shimamura C, Okuno Y, Yamato M, Harayama T

机构信息

Faculty of Pharmaceutical Sciences, Okayama University, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1997 Dec;45(12):2096-9. doi: 10.1248/cpb.45.2096.

DOI:10.1248/cpb.45.2096

PMID:9433781

Abstract

Indolo[3,2-b]quinoline derivatives (1b-i) with a methyl group at each possible position have been synthesized. The 1-methyl (1b) and 9-methyl (1i) derivatives were inactive, but the 3-methyl (1d), 4-methyl (1e), and 6-methyl (1f) derivatives exhibited high treatment/control (T/C) value and cure rates against leukemia P388 in mice. These results indicated that modification of indolo[3,2-b]quinoline derivatives at 3, 4, and 6 positions may be useful approach for lead optimization.

摘要

已合成了在每个可能位置都带有甲基的吲哚并[3,2 - b]喹啉衍生物（1b - i）。1 - 甲基（1b）和9 - 甲基（1i）衍生物无活性，但3 - 甲基（1d）、4 - 甲基（1e）和6 - 甲基（1f）衍生物在小鼠白血病P388模型中表现出高治疗/对照（T/C）值和治愈率。这些结果表明，在吲哚并[3,2 - b]喹啉衍生物的3、4和6位进行修饰可能是优化先导化合物的有效方法。