Design and Synthesis of A Ring C8 Substituent and C Ring C2 Oxygenated Pyrrolo[2,1-c][1,4]benzodiazepine as Anticancer Alkylating Agents

• Main Authors: Hua-Ping Chen, 陳華萍
• Other Authors: Jeh-Jeng Wang
• Format: Others
• Language: zh-TW
• Published: 2004
• Online Access: http://ndltd.ncl.edu.tw/handle/67780950548373491876

碩士 === 高雄醫學大學 === 醫藥暨應用化學系碩士班 === 92 === 英文摘要 Pyrrolo [ 2,1-c ] [ 1,4 ] benzodiazepines (PBDs) were isolated from streptomyces species and belong to an antitumour antibiotic. They can block DNA transcription . These compounds show their biological activity by binding selectively in the minor groove of DNA forming a covalent aminal bond between the C11 position of the PBD and the exocyclic N2 group of guanine base. In this thesis, we extended our studies to oxygen group incorporated at C-ring C-2 and modificated A-ring C-8 substituent of PBDs. We expected that these drugs may produce enhanced anticancer activity as potential DNA binding anticancer alkyling agents.