Synthesis of Novel Anticancer Agents

新型抗癌药物的合成

• 批准号: 6924636
• 负责人: Marisa C Kozlowski
• 金额: $ 19.82万
• 依托单位: UNIVERSITY OF PENNSYLVANIA
• 依托单位国家: 美国
• 财政年份: 2004
• 资助国家: 美国
• 起止时间: 2004-07-20 至 2008-04-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6924636
• 关键词: analog; antineoplastics; biological products; biotechnology; carbazoles; catalyst; chemical bond; chemical structure function; drug design /synthesis /production; flavones; method development; naphthoquinones; pharmacokinetics; quinones; stereoisomer

DESCRIPTION (provided by applicant): The potential for photodynamic cancer therapy with the perylenequinone and hypericin structural types is especially noteworthy given recent developments in this area. The proposed program focuses on synthesis of such complex natural products and their analogs by mimicking biological oxidative systems. Methods to form C-C bonds via oxidative C-H bond activation while establishing axial chirality will be developed using chiral oxidative catalysts. The possibility of selectivity in these transformations with respect to complex substrates is of significant synthetic potential. If such goals are realized, novel and unique synthetic strategies for the assembly of natural products can be envisioned. Routes to symmetric and dissymmetric chiral binaphthyl, perylenequinone, bisnaphthopyrone, bisanthraquinone, hypericin, and bisflavone natural products are presented.

描述（由申请人提供）：鉴于该领域的最新发展，佩里烯酮酮和甲基烯结构类型的光动力癌治疗的潜力尤其值得注意。提出的计划着重于通过模仿生物氧化系统的这种复杂天然产物及其类似物的综合。通过手性氧化催化剂开发通过氧化C-H键激活形成C-C键的方法。在这些转化中相对于复杂底物的选择性的可能性具有显着的合成潜力。如果实现此类目标，则可以设想为组装天然产品的新颖和独特的合成策略。提出了与对称和非对称性手性双吡啶酮，per烯酮，双胃吡啶酮，双足酮，双丝钟和双氟酮天然产物的途径。