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題 名 | 設計及合成8-胺基比咯苯偶氮駢混成抗癌試劑=Design and Synthesis of 8-Amino-pyrrolo-[2,1-c][1,4]benzodiazepine Hybrid Agents |
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作 者 | 蔡平賜; 王志鉦; 吳瑞泰; | 書刊名 | 高雄應用科技大學學報 |
卷 期 | 31 2001.12[民90.12] |
頁 次 | 頁45-61 |
分類號 | 418.31 |
關鍵詞 | 比咯苯偶氮駢; 抗癌活性; 序列選擇性; 烷化試劑; Pyrrolo[2,1-c]benzodiapines; Antitumor-activity; Sequence-selectivity; Alkylating agent; |
語 文 | 中文(Chinese) |
中文摘要 | 由鏈黴菌所屬所產生之比咯苯偶氮駢(PBDs),雖能共價鏈結於DNA窄溝槽之鳥糞嘌呤guanine氮2位置而有抗癌活性,但由於會導致一些副作用,在臨床應用上便受到了限制。所以近來研究都著重於繼續增加其抗癌活性並提高其序列選擇性;文獻上一些新型雙效PBD混成試劑及PBD二聚物陸續的被提出,然而至今尚未有在PBD的A環上碳8位置為胺基的PBD化合物或衍生物被合成出。 本篇論文之目的即在合成出新型的8-胺基PBD二聚物,並期望這些試劑能提供較高的抗癌活性及序列選擇性。 |
英文摘要 | The Pyrrolo[2,1-c]benzodiapines (PBDs) produced by the stretomyces, could covalent-bind to N-2 guanine within the minor groove of DNA. Although these drugs show potent antitumor activity, their clinical application has been limited due to their side effects. The objectives of this thesis are to design and synthesize new types of PBDs hybride agents based upon 8-Amino PBD coupled with indole moieties. (2S)-Pyrrolidine-2-carbaldehyde-diethylthioacteal (PCT)(7) was synthesized with six steps from L-proline (1) in 41.6% yield. Then compound (7) reacted with 2,4-dinitrobenzo nic acid to give (2S)-N-(2,4- dinitrobenzoyl) pyrrolidine -2-carbaldehyde-diethylthioacetal (8), followed by reduction with indium to generate (2S)-N-(2,4- diaminobenzoyl) pyrro lidine-2-carbaldehydediethylthioacetal (9) with two steps in 56% yield. The remaining two steps, cycliczation of compound (10) and dimerization at N-8 with different carbon chain length, are well precedented, and should present no insurmountable problems. Targe product 8-(Propylamino)-10-methoxymethyl-pyrrolo[1,4]benzodiazepine-5,10-dione DIMER (19) was synthesize with five steps from 4-nitro-2-amino benzo- nic acid in 14% yield. Antitumor activity will be achieved in the further study. |
本系統中英文摘要資訊取自各篇刊載內容。