COMBINATORIAL LIBRARIES BASED ON DOLASTATIN 10

描述：(改编自申请者的摘要) 项目是优化固有的细胞毒性和抗肿瘤 在第一阶段，作者将开发一种 经Evans Aldol修饰的化合物的固相合成 技术向固相转化。然后他们将使用组合式 化学应用该方法合成320个类似物并进行筛选 它们用于抑制微管蛋白聚合和细胞毒性。任何 这样确定的线索将被用于设计后续的聚焦 图书馆。候选化合物将在 与制药合作伙伴的合作。 建议的商业应用：不可用

DESCRIPTION: (Adapted from the applicant's abstract) The goal of the project is to optimize the inherent cytotoxicity and antineoplastic activity of dolastatin 10. In phase I, the authors will develop a solid-phase synthesis of the compound by adaptation of the Evans aldol technology to the solid phase. They will then use combinatorial chemistry to apply the method to synthesizing 320 analogs and screen them for inhibition of tubulin polymerization and cytotoxicity. Any leads thus identified will be used to design subsequent focused libraries. Candidate compounds will undergo further testing in collaboration with a pharmaceutical partner. PROPOSED COMMERCIAL APPLICATION: NOT AVAILABLE