AUTOMATED SYNTHESIS OF A COMBINATORIAL LIBRARY

描述：(改编自申请人的摘要)固相 科学公司(SPSC)提议制作一个组合库 取代的吖啶和吡啶类似物的抗癌作用 放映。该库将由每个5毫克组成，总共 640个单独的化合物。SPSC将通过利用它的 新型高负荷顺磁支架和新研制的自动化 反应全会。具体地说，图书馆将利用这种高- 装载支持，将所需产品从可溶产品中分离 反应混合物的组成。后续结构--活动-- 由50-100个化合物组成的关系(SAR)库也将 根据640化合物文库的筛选结果制作。 第二阶段工作的目标将是完成 新的自动反应全压室同时生产由以下组成的库 一系列以吖啶和吡啶为基础的杂环化合物的合成 在国家癌症研究所进行癌症筛查。 建议的商业应用： 一种商品化的药物自动组合文库合成器 发现号。

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.