5,6-二甲基-9-甲氧基-1-苯基-6H-吡啶并[4,3-b]咔唑衍生物的合成及其细胞毒性活性。

Synthesis of 5,6-dimethyl-9-methoxy-1-phenyl-6H-pyrido[4,3-b]carbazole derivatives and their cytotoxic activity.

作者信息

Jasztold-Howorko Ryszard, Pelczynska Marzena, Nasulewicz Anna, Wietrzyk Joanna, Opolski Adam

机构信息

Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Wroclaw, Poland.

出版信息

Arch Pharm (Weinheim). 2005 Nov;338(11):556-61. doi: 10.1002/ardp.200500141.

DOI:10.1002/ardp.200500141

PMID:16281305

Abstract

Starting from 2-(6-methoxy-1-methyl-9H-carbazol-2-yl)ethylamine 7 and mixed anhydrides of 4-nitrobenzoic acid or 4-methoxybenzoic acid, the corresponding 5,6-dimethyl-9-methoxy-1-(4-substituted phenyl)-6H-pyrido[4,3-b]carbazoles 11a-b, 5,6-dimethyl-9-hydroxy-1-(4-substituted phenyl)-6H-pyrido[4,3-b]carbazoles 12a, 12c, and their quaternary salts 13a-d were obtained. The four new pyridocarbazole derivatives 12a-c and 13d satisfy the international activity criterion for synthetic compounds, namely an ID(50) value lower then 4 microg/mL in preliminary in vitro cytotoxic activity screening against the A549 cell line (non-small cell lung cancer).

摘要

从2-(6-甲氧基-1-甲基-9H-咔唑-2-基)乙胺7与4-硝基苯甲酸或4-甲氧基苯甲酸的混合酸酐出发，得到了相应的5,6-二甲基-9-甲氧基-1-(4-取代苯基)-6H-吡啶并[4,3-b]咔唑11a - b、5,6-二甲基-9-羟基-1-(4-取代苯基)-6H-吡啶并[4,3-b]咔唑12a、12c及其季铵盐13a - d。四种新的吡啶并咔唑衍生物12a - c和13d符合合成化合物的国际活性标准，即在针对A549细胞系（非小细胞肺癌）的初步体外细胞毒性活性筛选中ID(50)值低于4μg/mL。