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: 13672338
• 负责人: KURIHARA Masaaki
• 金额: $ 2.24万
• 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: 2001
• 资助国家: 日本
• 起止时间: 2001 至 2002
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-13672338/
• 关键词: enediyne; Bergman reaction; trigger; DNA cleavage; 光照射

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.Kurihara, M.Tanaka, M.Oba, H.Suemune: "Computational Study on Conformation of Oligopeptides Containing Chiral alpha, alpha-Disubstituted Amino Acids"Peptides 2002. 786-787 (2003)

M.Kurihara、M.Tanaka、M.Oba、H.Suemune：“含有手性 α、α-二取代氨基酸的寡肽构象的计算研究”肽 2002. 786-787 (2003)

I.Nakanishi, K.Fukuhara, K.Ohkubo, T.Shimada, H.Kansui, M.Kurihara, S.Urano, S.Fukuzumi, N.Miyata: "Superoxide Anion Generation via Electron-Transfer Oxidaition of Catechin Dianion by Molecular Oxygen in an Aprotic Medium"Chem. Lett.. 2001. 1152-1153 (200

I.Nakanishi、K.Fukuhara、K.Ohkubo、T.Shimada、H.Kansui、M.Kurihara、S.Urano、S.Fukuzumi、N.Miyata：“通过儿茶素二价阴离子的电子转移氧化产生超氧阴离子

A. Kittaka, M. Kurihara, S. Peleg, Y. Suhara, H. Takayama: "2α-(3-Hydroxypropyl)- and 2α-(3-Hydroxypropoxy)-1α,25-vitamin D3 Accessible to Vitamin D Receptor Mutant Related to Hereditary Vitamin D-Resistant Rickets"Chem. Pharm.Bull.. 51. 357-358 (2003)

A. Kittaka、M. Kurihara、S. Peleg、Y. Suhara、H. Takayama：“2α-(3-羟丙基)-和 2α-(3-羟丙氧基)-1α,25-维生素 D3 可与维生素 D 受体突变体接触与遗传性维生素 D 抗性佝偻病相关的《Chem. Pharm. Bull.. 51. 357-358 (2003)》

M.Kurihara, W.Hakamata: "Convenient Preparation of Cyclic Acetals Using Diols, TMS-source and a Catalytic Amount of TMSOTf"J.Org.Chem.. 68. 3413-3415 (2003)

M.Kurihara、W.Hakamata：“使用二醇、TMS 源和一定量的 TMSOTf 方便地制备环状缩醛”J.Org.Chem.. 68. 3413-3415 (2003)

M.Oba, M.Tanaka, M.Kurihara, H.Suemune: "Conformation of Peptides Containing a Chiral α-Ethylated α,α-Disubstituted α-Amino Acid : (S)-EthylLeucine (= (2S)-2-Amino-2-ethyl-4-methylpentanoic Acid) within Sequences of Dimethylglycine and Diethylglycine Resi

M.Oba、M.Tanaka、M.Kurihara、H.Suemune：“含有手性 α-乙基化 α,α-二取代 α-氨基酸的肽的构象：(S)-乙基亮氨酸 (= (2S)-2-氨基-2-乙基-4-甲基戊酸）在二甲基甘氨酸和二乙基甘氨酸残基序列中