MOLECULAR DESIGN AND SYNTHESIS OF A NEW CLASS OF TRIGGERED ENEDIYNE

一类新的触发烯的分子设计与合成

• 批准号: 11672223
• 负责人: KURIHARA Masaaki
• 金额: $ 1.92万
• 依托单位: NATIONAL INSTITUTE OF HEALTH SCIENCES
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 1999
• 资助国家: 日本
• 起止时间: 1999 至 2000
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-11672223/
• 关键词: enediyne; Bergman reaction; trigger; DNA cleavage

It is an interesting challenge to design alternate frameworks and triggering mechanisms, with the goal of producing a stable enediyne which can be activated under controlled conditions, especially in away which directs the cytotoxicity toward a specific pathogen or tissue.I found simple trigger of cycloaromatization in enediyne system. This enediyne compound were activated by deprotection to cleave DNA.

这是一个有趣的挑战，设计替代框架和触发机制，与目标是生产一个稳定的烯二炔，可以在受控条件下激活，特别是在远离直接细胞毒性对特定的病原体或组织。该烯二炔化合物通过去保护而活化以切割DNA。

项目成果

M.Tanaka,M.Oba,N.Imawaka,Y.Tanaka,M.Kurihara,H.Suemune: "Cnoformational Study of Heteropentapeptides Containing an α-Ethylated α,α-Disubstituted Amino Acids : (S)-Butylethylglycine (=2-Amino-2-ethylhexanoic Acid) within Dimethylglycine (= 2-Aminoisobutyri

M.Tanaka、M.Oba、N.Imawaka、Y.Tanaka、M.Kurihara、H.Suemune：“含有 α-乙基化 α,α-二取代氨基酸的杂五肽的形态学研究：(S)-丁基乙基甘氨酸 (=2) -氨基-2-乙基己酸）二甲基甘氨酸（= 2-氨基异丁酸）

M.Kurihara,M.N.Miyata,Tanaka,N.Imawaka,H.Suemune: "Conformational Analysis of Homooligopeptides Prepared From Isovaline and Diethylglycine : Molecular Mechanics Study"JCPE Journal. 11. 185-190 (1999)

M.Kurihara、M.N.Miyata、Tanaka、N.Imawaka、H.Suemune：“异缬氨酸和二乙基甘氨酸制备的同寡肽的构象分析：分子力学研究”JCPE 杂志。

S.Kobayashi,H.Kobayashi,T.Yamaguchi,M.Nishida,K.Yamaguchi,M.Kurihara,N.Miyata,A.Tanaka: "Synthesis,Conformation, and Chemical Properties of New Mini Parallel Double-Stranded Peptides Conjugated with -Phe-Phe- and -Phe-Phe-X- Sequences"Chem.Pharm.Bull.. 48

S.Kobayashi,H.Kobayashi,T.Yamaguchi,M.Nishida,K.Yamaguchi,M.Kurihara,N.Miyata,A.Tanaka：“新型微型平行双链肽的合成、构象和化学性质

A.Nishikawa,F Furukawa,K.Kasahara,S.Ikezaki,T.Itoh,T.Suzuki,K.Uchida,M.Kurihara,M.Hayashi,N.Miyata,M.Hirose: "Trans-4-hydroxy-2-nonenal, an aldehydic lipid peroxidation product, lacks genotoxicity in lacI transgenic mice."Cancer Lett.. 148. 81-86 (2000)

A.Nishikawa、F Furukawa、K.Kasahara、S.Ikezaki、T.Itoh、T.Suzuki、K.Uchida、M.Kurihara、M.Hayashi、N.Miyata、M.Hirose：“Trans-4-羟基-

M.Tanaka,M.Oba,N.Imawaka,Y.Tanaka,M.Kurihara,H.Suemune: "Cnoformational Study of Heteropentapeptides Containing an α-Ethylated α,α-Disubstituted Amino Acids : (S)-Butylethylglycine (=2-Amino-2-ethylhexanoic Acid) within Dimethylglycine (=2-Aminoisobutyric

M.Tanaka、M.Oba、N.Imawaka、Y.Tanaka、M.Kurihara、H.Suemune：“含有 α-乙基化 α,α-二取代氨基酸的杂五肽的形态学研究：(S)-丁基乙基甘氨酸 (=2) -氨基-2-乙基己酸）二甲基甘氨酸（=2-氨基异丁酸）