COMBINATORIAL LIBRARIES BASED ON DOLASTATIN 10

描述：（改编自申请人的摘要） 该项目是为了优化固有的细胞毒性和生物相容性， 多拉司他汀的活性10. 在第一阶段，作者将开发一个 通过调整Evans醛醇来固相合成化合物 技术到固相。 然后他们将使用组合 化学应用该方法合成320个类似物并筛选 它们用于抑制微管蛋白聚合和细胞毒性。 任何 由此确定的线索将用于设计随后的重点 图书馆. 候选化合物将在2015年进行进一步测试。 与制药合作伙伴合作。 拟议商业应用：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