Design and Synthesis of Anticancer Alkylating Agents of Pyrrolo[2,1-c][1,4]benzodiazepine Containing Oxygen Group in C-ring
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 DN...
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| Format: | Others |
| Language: | zh-TW |
| Published: |
2003
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| Online Access: | http://ndltd.ncl.edu.tw/handle/4a6nuu |
| Summary: | 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.
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