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新型橄榄枝碱衍生物的合成及其构效关系分析

Synthesis and structure-activity relationship analysis of new olivacine derivatives.

作者信息

Tylińska Beata, Jasztold-Howorko Ryszard, Mastalarz Henryk, Kłopotowska Dagmara, Filip Beata, Wietrzyk Joanna

机构信息

Wrocław Medical University, Faculty of Pharmacy, Department of Organic Chemistry, Grodzka 9, 50-137 Wrocław, Poland.

出版信息

Acta Pol Pharm. 2010 Sep-Oct;67(5):495-502.

Abstract

The number of 3'- and 4'-substituted 1-phenyl-6H-pyrido[4,3-b]carbazole derivatives have been synthesized and tested biologically. Eleven of the newly obtained compounds were subjected to the preliminary cytostatic screening for their activity against L1210 (murine leukemia), A498 (human kidney cancer), A549 (human lung cancer) and HT29 (human colon cancer) cell lines. Eight of tested derivatives exhibited significant biological activities, which only weakly depended on side chain length and position of the substituent.

摘要

已合成了多种3'-和4'-取代的1-苯基-6H-吡啶并[4,3-b]咔唑衍生物,并进行了生物学测试。对新获得的11种化合物针对L1210(小鼠白血病)、A498(人肾癌)、A549(人肺癌)和HT29(人结肠癌)细胞系的活性进行了初步的细胞生长抑制筛选。8种测试衍生物表现出显著的生物学活性,其活性仅微弱地依赖于侧链长度和取代基的位置。

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