Total Synthesis of Bioactive Natural Products

生物活性天然产物的全合成

• 批准号: 6698021
• 负责人: EMMANUEL A THEODORAKIS
• 金额: $ 20.01万
• 依托单位: UNIVERSITY OF CALIFORNIA, SAN DIEGO
• 依托单位国家: 美国
• 财政年份: 2001
• 资助国家: 美国
• 起止时间: 2001-03-01 至 2006-02-28
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6698021
• 关键词: angiogenesis inhibitors; antineoplastics; carboxylation; chemical addition; chemical synthesis; cyclopentane; diterpenes; drug design /synthesis /production; macrolide antibiotics; quinones; reverse transcriptase inhibitors; sesquiterpenes

DESCRIPTION: (Applicant's Description) The first objective of this proposal is to study a novel methodology that allows access to substituted quinones and evaluate its scope and limitations during the synthesis of bioactive natural products, such as ilimaquinone avarone and avarol. The second objective of this proposal is the synthesis of norrisolide, a natural product for which in vivo studies have demonstrated that it causes irreversible vesiculation of the Golgi complex. A third objective of our research is the synthesis of borrelidin, an unusual macrolide with a very potent profile as an angiogenesis inhibitor.

说明：（申请人的说明）本提案的第一个目的是 研究一种新的方法，可以获得取代的醌， 评价其范围和限制在生物活性天然合成 产品，如靛醌avarone和avarol。第二个目标是 建议是合成norrisolide，一种天然产物， 研究表明，它会导致高尔基体不可逆的囊泡形成 复杂.我们研究的第三个目标是合成疏螺旋体素， 一种不寻常的大环内酯类药物，具有非常有效的血管生成抑制剂作用。