A10: SYNTHESIS OF NON NUCLEOSIDIC ANTIVIRAL AGENTS: HIV & CANCER DRUG DESIGN

A10：非核苷类抗病毒药物的合成：HIV

• 批准号: 6205929
• 负责人: STANLEY L EVANS
• 金额: $ 3.09万
• 依托单位: MEHARRY MEDICAL COLLEGE
• 依托单位国家: 美国
• 财政年份: 1999
• 资助国家: 美国
• 起止时间: 1999-09-30 至 2000-09-29
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6205929
• 关键词: AIDS; biological products; biotechnology; drug /agent; hematology; immunology; infection; inflammation; lymphatic system; minority institution research support; structural biology; virus

The design, synthesis and evaluation of antiviral agents of the non-nucleosidic type remain the major goal of this research project. Our lead compound 2,3-diveratryl-3-chloropropenal (compound 1) and active antiviral agent serves as a starting point for structural activity relationships. (SAR) for drug design. Compound 1 contains the alpha, beta unsaturated carbonyl group in its molecular structure. We used this unsaturated carbonyl group as a combinational starting point for new medicinal entities. Chalcones the un-cyclic precursor to flavonoids, contain the alpha, beta unsaturated carbonyl group in its chemical structure. Chalcones have been shown to express antiproliferative activity by a number of investigators. Leinamycin, an antibiotic with antitumor activity, contains an extended unsaturated (alpha, beta, gamma, delta) carbonyl group in its chemical structure. Although a significant amount of antitumor activity is associated with the 1,2 diethylene-3-oxide group of the leinamycin molecule, it cannot account for all of its antitumor action. We suggest that the alpha, beta, gamma, delta unsaturated carbonyl group also contributes to leinamycin antitumor activity.

抗病毒药物的设计、合成及评价 非核苷型仍然是该研究项目的主要目标。 我们的先导化合物 2,3-diveratryl-3-氯丙烯醛（化合物 1）和 活性抗病毒剂作为结构的起点 活动关系。 （SAR）用于药物设计。 化合物1含有 其分子结构中含有α、β不饱和羰基。 我们使用这个不饱和羰基作为组合起始 新药物实体的点。 查耳酮非环状前体 黄酮类化合物中含有α、β不饱和羰基 它的化学结构。 查耳酮已被证明可以表达 许多研究人员的抗增殖活性。 莱纳霉素， 一种具有抗肿瘤活性的抗生素，含有延长的 其化学中不饱和（α、β、γ、δ）羰基 结构。 虽然大量的抗肿瘤活性 与莱那霉素的 1,2 二亚乙基-3-氧化物基团相关 分子，它不能解释其所有的抗肿瘤作用。 我们 表明 α、β、γ、δ 不饱和羰基 还有助于莱那霉素的抗肿瘤活性。