CYTOTOXIC MACROCYCLES CYTOCHALASIN PYRROLIZIDINE ANALOGS

细胞毒性大环细胞松弛素吡咯利嗪类似物

• 批准号: 3164806
• 负责人: EDWIN VEDEJS
• 金额: $ 21.52万
• 依托单位: UNIVERSITY OF WISCONSIN-MADISON
• 依托单位国家: 美国
• 财政年份: 1978
• 资助国家: 美国
• 起止时间: 1978-07-01 至 1990-12-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3164806
• 关键词: Retroviridae; Retroviridae disease; antineoplastics; biological transport; cell membrane; chelating agents; cytochalasins; cytotoxicity; drug design /synthesis /production; drug screening /evaluation; leukocyte antigen typing; membrane activity; monocrotaline; neoplasm /cancer pharmacology; neoplastic transformation; nitrogen compounds; sulfur compounds; tissue /cell culture; virus infection mechanism; virus replication

The isoindolone fragment of cytochalasin D has been assembled by Diels-Alder reaction of an optically active N-benzoyl pyrrolinone intermediate with a substituted diene. This intermediate will be taken on to analogs of cytochalasin D by a ring expansion sequence where a 6-membered sulfide ring is bridged across the alpha, alpha' positions by a 6-carbon chain. The result of this reaction would be to complete the 11-membered carbocyclic periphery of cytochalasin D.

细胞松弛素D的异吲哚片段已由Diels-Alder组装 光学活性N-苯甲酰基吡咯烷酮中间体与 取代二烯。这个中间体将被用来模拟 细胞松弛素D通过环扩展序列，其中6元硫环是 通过一个6-碳链连接在α，α‘位置上。其结果是 这个反应将完成11个成员的碳环外围 细胞松弛素D。