設計與合成C環衍生物之比咯苯偶氮駢抗癌烷化試劑

Design and Synthesis of Anticancer Alkylating Agents of Pyrrolo[2,1-c][1,4]benzodiazepine in C-ring-modified analogues

林苗均(Miao-Chun Lin)

指導教授 ： 王志鉦

高雄醫學大學/生命科學院/化學系/碩士(2003年)

摘要

比咯苯偶氮駢（pyrrolo[2,1-c][1,4]benzodiazepines ， PBDs）是由鏈球菌屬所分離出來的一種很強的抗癌試劑和基因導向試劑（gene-target agents）。藥物學家與化學家已設計合成出許多具有PBDs結構的DNA烷化試劑，大部份的研究都是在A環的C6、C7、C8和C9位置上進行衍生化反應，或者在A環的C7位置上用長鏈連結而成PBDs的複合物（PBDs dimer），如DSB-120。本論文提出不同的設計方向，設計合成在C環上C2位置不同取代的PBDs抗癌烷化試劑，以期提高對DNA的選擇性與抗癌活性。

關鍵字

比咯苯偶氮駢抗癌烷化試劑

並列摘要

pyrrolo[2,1-c][1,4]benzodiazepines（PBDs）are a group of potent naturally occurring antibiotics antitumour agents produced by various Streptomyces species. In the past, most of investigations of PBDs have been focus on the synthesis of the PBD monomers by modification of C6, C7, C8 and C9 positions of A-ring or linked by crosslinking agents at C7 position of PBD monomers. However, in this study, we prepared a new PBDs, which contains an amino group at C2 position of C-ring to enforce the DNA selectivity and to increase the antitumor activity.

並列關鍵字

none

參考文獻

參考文獻

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