The Total Synthesis of fleephilone

弗菲酮的全合成

• 批准号: 6739288
• 负责人: ERIC M FLAMME
• 金额: $ 4.11万
• 依托单位: PRINCETON UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2004
• 资助国家: 美国
• 起止时间: 2004-04-01 至 2007-03-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6739288
• 关键词: antiAIDS agent; antiviral agents; biotherapeutic agent; butyrates; chemical synthesis; cyclic compound; drug design /synthesis /production; human immunodeficiency virus 1; organic chemicals; postdoctoral investigator; protein binding; quinolizine; stereochemistry; virus protein; virus replication

DESCRIPTION (provided by applicant): The broad and long term objective of this proposal is to synthesize the natural product fleephilone in order to elucidate how fleephilone inhibits REV/RRE binding between the REV protein and mRNA in the HIV-1 Virus. Inhibition of REV/RRE binding is a viable target for a research program focused on the prevention of HIV-1 replication. Inhibition studies will be carried out using NMR techniques to study exactly how fleephilone interrupts binding. With a greater understanding of how fleephilone inhibits REV/RRE binding it is anticipated that more potent analogs of fleephilone can be synthesized in an effort to develop AIDS drugs targeting REV/RRE binding. The specific aims of the proposal are to synthesize the natural product fleephilone using techniques in organic synthetic chemistry. The total synthesis of fleephilone will also allow for the determination of the absolute and relative stereochemistry of the molecule.

描述（由申请人提供）：本提案的广泛和长期目标是合成天然产物fleephilone，以阐明fleephilone如何抑制HIV-1病毒中REV蛋白和mRNA之间的REV/RRE结合。抑制REV/RRE结合是一个可行的目标，为一个研究计划，重点是预防HIV-1复制。将使用NMR技术进行抑制研究，以确切研究fleephilone如何中断结合。随着对fleephilone如何抑制REV/RRE结合的更深入了解，预期可以合成更有效的fleephilone类似物，以开发靶向REV/RRE结合的AIDS药物。该提案的具体目标是使用有机合成化学技术合成天然产物fleephilone。fleephilone的全合成也将允许确定分子的绝对和相对立体化学。