BORADEOXYRIBONUCLEOSIDES

硼脱氧核糖核苷

• 批准号: 3304370
• 负责人: DONALD S MATTESON
• 金额: $ 9.38万
• 依托单位: WASHINGTON STATE UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1990
• 资助国家: 美国
• 起止时间: 1990-06-05 至 1993-05-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3304370
• 关键词: antiAIDS agent; antineoplastics; antiviral agents; boron; chemical structure function; deoxyribonucleosides; drug design /synthesis /production; drug screening /evaluation; nucleic acid chemical synthesis; nucleoside analog

"Boradeoxyribonucleosides" focuses on two points where boron may replace carbon in deoxyribonucleosides to provide novel compounds which have a good chance of being antiviral agents. First, syntheses of 3-[1-(2- deoxy)ribosyl]-6-borapyrimidines are proposed. 6-Borapyrimidines are the only borapyrimidine isomers which have the boron atom in a hydrolytically stable position. This is a significant series of compounds to test because there are only a limited number of ways in which the pyrimidine ring can be modified so as to interfere with RNA or DNA synthesis. Syntheses of deoxyribonucleoside analogues having boron substituents in the 3-position of the deoxyribose unit are also proposed. These bear a close structural analogy to known anti-HIV-1 agents such as AZT or DDC and would be likely to decouple the crucial enzymatic phosphorylation for nucleotide synthesis. ONce the compounds have been prepared, samples will be submitted for screening against the AIDS virus. Samples will also be screened for anticancer activity, as well as for other antiviral activity. If nontoxic compounds are found, they will be submitted elsewhere for screening as possible agents for the proposed 10B neutron capture tumor therapy.

“硼脱氧核糖核苷”主要关注硼可能取代的两个点