設計與合成比咯苯偶氮駢抗癌烷化結合試劑及C環含硫基衍生物

Design and Synthesis of Anticancer Alkylating Agents of Pyrrolo[2,1-c][1,4]benzodiazepines Hybrid Agents and Containing Sulfur Group in C-ring Analogues

沈煜凱(Yu-Kai Shen)

指導教授 ： 王志鉦

高雄醫學大學/生命科學院/醫藥暨應用化學研究所/碩士(2005年)

摘要

中文摘要 :
比咯苯偶氮駢（PBDs），是由鏈黴素所產生的與DNA結合抗癌抗生素。這類藥物可與DNA次溝槽的鳥糞瞟呤共價鍵結，阻礙DNA的複製，達到抗癌效果。在本論文中，將分兩部分討論。一、我們設計合成在C環位置上，導入含硫的長碳鏈結構，以期提高對DNA的選擇性及抗癌活性。二、DC81這類化合物與Indole carboxylate(IC)的結合試劑作為抗癌藥，這些藥物皆具很好的生物活性，我們使用不同IC與DC81鍵結，已送至美國NCI，期望有良好的抗癌活性。

關鍵字

設計與合成比咯苯偶氮駢抗癌烷化結合試劑及C環含硫基衍生物

並列摘要

英文摘要 :
The pyrrolo [2,1-C] [1,4] benzodiazepines (PBDs), a family of potent DNA-binding antitumor antibiotic are produced by streptomyces species. The PBDs can interact with DNA in a sequence – selective fashion, and form a covalent bond with a guanine base in the minor groove of DNA. This adduct formation is thought to lead to the observed biological activity.
In this dissertation, we focused on two area. First, we synthesized new PBDs, which contain a sulfur group at C2 position of C-ring to try to increase the DNA sequence selectivity and the antitumor activity. Second, the DC81 and indole carboxylate (IC) hybrid agent has shown highly anticancer activity. We further investigated this type of hybrid agents. One of them has been synthesized and sent to NCI for screening test. We expected this hybrid agent have highly biological activity.

並列關鍵字

Design and Synthesis of Anticancer Alkylating Ag ； 1-c][1 ； 4]benzodiazepines Hybrid Agents and Containing S

參考文獻

七、參考文獻：

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