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

• Main Authors: Yen-Chi Chen, 陳彥吉
• Other Authors: Jeh-Jeng Wang
• Format: Others
• Language: zh-TW
• Published: 2003
• Online Access: http://ndltd.ncl.edu.tw/handle/4a6nuu

碩士 === 高雄醫學大學 === 天然藥物研究所 === 91 === DC-81 , an antitumor antibiotic produced by streptomyces species, belogs to the pyrrolo[2,1-c][1,4]benzodiazepines (PBDs) which are potent inhibitors of nucleic acid synthesis and block DNA transcription. They bind selectively in the minor groove of DNA forming a covalent aminal bond between the C11 position of the central B-ring and the N2 amino group of a guanine base. This adduct formation is thought to lead to the observed biological activity. Recently, we reported a very short route and large scale synthesis of PBD. In this dissertation, we extended our studies to oxygen group incorporated at C-ring of PBD. Biological test showed that these drugs have highly anticancer activity.