PHENOLIC SUBSTITUTED LIGANDS FOR DIAGNOSIS AND THERAPY

用于诊断和治疗的酚取代配体

• 批准号: 3752343
• 负责人: M W BRECHBIEL
• 金额: --
• 依托单位: DIVISION OF CANCER TREATMENT
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/3752343
• 关键词: carboxylate; chelating agents; chemical binding; chemical kinetics; chemical stability; chemical substitution; chemical synthesis; diagnostic tests; ligands; metal complex; molecular site; neoplasm /cancer radiation therapy; neoplasm /cancer radiodiagnosis; phenols; thermodynamics

The principal objective of this project was to obtain an understanding of the fundamental coordination chemistry of polyaminocarboxylate ligands which have had one or more carboxylates replaced with a phenolate metal binding site. Thus, synthesis of a series of novel acyclic ligands of various substitution patterns was required. Information acquired from evaluation of the solution chemistry of these compounds, their kinetic and thermodynamic properties, and their serum stability have been employed to gauge the potential usefulness of the complexes in vivo. These studies have provided a basis for rational design of bifunctional ligands for complexing metals useful as cytocidal or diagnostic agents. Results of the above studies have indicated that in and of themselves, the ortho-hydroxybenzyl metal binding site, when incorporated into a polyaminocarboxylate ligand, does not provide an adequately stable complex in vivo. However, the knowledge gained from the syntheses provides rational synthetic routes to analogous thiophenolic type ligands and as such, this project will be incorporated into project number Z0l CM 06399- 03 RO.

该项目的主要目标是了解 聚氨基辅助配体的基本协调化学 用一个或多个羧酸盐代替了苯甲酸酯 绑定位点。 因此，一系列新型的无环配体的合成 需要各种替代模式。 从中获取的信息 评估这些化合物的溶液化学，它们的动力学和 热力学特性及其血清稳定性已采用 衡量体内复合物的潜在有用性。 这些研究为双功能的合理设计提供了基础 络合金属的配体有用，可作为细胞固体或诊断剂。 以上研究的结果表明，在本身中 当纳入邻苯甲苯苯甲酰金属结合位点 聚氨基辅助配体，不提供足够稳定的复合物 体内。 但是，从合成中获得的知识提供了 与类似硫苯酚型配体的有理合成路线和AS 这样的项目将纳入项目编号Z0L CM 06399- 03 RO。