咔唑基-1,2,3,4四氫-β-卡林與咔唑基-3,4二氫-β-卡林衍生物及其製備方法

專利類型

發明

專利國別 (專利申請國家)

中華民國

專利申請案號

100128232

專利證號

I 462921

專利獲證名稱

咔唑基-1,2,3,4四氫-β-卡林與咔唑基-3,4二氫-β-卡林衍生物及其製備方法

專利所屬機關 (申請機關)

國立臺灣大學

獲證日期

2014/12/01

技術說明

本發明係關於一種新穎的化合物或其醫藥組成物及其製造方法，該化合物具有如下結構式。該化合物具有顯著和/或選擇性的細胞毒殺活性，且具有高度潛力可發展成拓撲酶抑制劑。本發明應用N烷化反應(N-alkylation)、達夫反應(Duff reaction，又稱六亞甲基四胺甲醯化反應)、皮克特－施彭格勒反應(Pictet-Spengler reaction) 與 2,3-二氯-5,6-二氰對苯醌(2,3-dichloro-5,6-dicyanobezoquinone, DDQ)氧化反應等輕便的合成方法可成功製備Manzamines的類似物。 The present invention provides a novel compound/ pharmaceutical composition and a method for preparing the same. The compound/pharmaceutical composition includes the following formula. The compounds exhibit significant and/or selective cytotoxic activity and are potent inhibitors of DNA topoisomerse. A series of 1-substituted carbazole 1,2,3,4-tetrahydro- and carbazole 3,4-dihydro--carboline analogs have been synthesized and evaluated for antitumor activity against human tumor cells including KB, DLD, NCI-H661, Hepa, and HepG2/A2 cell lines. Among them, compounds 2, 6, 7, and 9 exhibited most potent and selective activity against tested tumor cells. As for inhibition of topoisomerase II, compounds 1-14 and 18 showed activity better than etoposide. Among them, compound 3, 4, 7, 9, and 10 exhibited potent activity.

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