AUTOMATED SYNTHESIS OF A COMBINATORIAL LIBRARY

组合库的自动合成

• 批准号: 2717492
• 负责人: IRVING SUCHOLEIKI
• 金额: $ 42.22万
• 依托单位: SOLID PHASE SCIENCES CORPORATION
• 依托单位国家: 美国
• 财政年份: 1998
• 资助国家: 美国
• 起止时间: 1998-08-10 至 2000-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/2717492
• 关键词: acridines; analog; analytical chemistry; antineoplastics; bioengineering /biomedical engineering; biomedical automation; biomedical equipment development; chemical registry /resource; chemical structure function; chemical substitution; chemical synthesis; computer program /software; drug screening /evaluation; heterocyclic compounds; high performance liquid chromatography; mass spectrometry; nuclear magnetic resonance spectroscopy; pyridine; robotics; solid state; ultrasound

DESCRIPTION: (Adapted from the applicant's abstract) Solid Phase Sciences Corporation (SPSC) proposes to produce a combinatorial library of substituted acridine and pyridine based analogs for anti-cancer screening. The library will consist of 5 milligrams each of a total of 640 individual compounds. SPSC will accomplish this by utilizing it's novel high-loading paramagnetic support and a newly developed automated reaction plenum. Specifically, libraries will be made off of this high- loading support to separate the desired products from the soluble components of the reaction mixture. A follow-up structure-activity- relationship (SAR) library composed of 50-100 compounds will also be produced based on the screening results of the 640 compound library. The goal of the Phase II effort will be to complete the development of the new automated reaction plenum while producing a library composed of a series of acridine and pyridine based heterocyclic compounds for anti cancer screening at the National Cancer Institute. PROPOSED COMMERCIAL APPLICATION: A commercial automated combinatorial library synthesizer for drug discovery.

描述：（改编自申请人摘要）固相 科学公司（SPSC）提出了一个组合库， 用于抗癌的取代的吖啶和吡啶基类似物 筛选图书馆将包括5毫克，每一个总共有 640种化合物。 SPSC将通过利用其 新型高负载顺磁性载体和新开发的自动化 反应室具体来说，图书馆将由这个高- 将所需产物与可溶性物质分离 反应混合物的组分。 一个后续的结构-活动- 由50-100种化合物组成的SAR库也将被 基于640化合物文库的筛选结果产生。 第二阶段工作的目标是完成 新的自动化反应室，同时产生一个库， 一系列基于吖啶和吡啶的杂环化合物， 国家癌症研究所的癌症筛查。 拟定商业应用： 一种商业化的自动化药物组合文库合成仪 的发现