PHENOLIC SUBSTITUTED LIGANDS FOR DIAGNOSIS AND THERAPY

用于诊断和治疗的酚取代配体

• 批准号: 5201266
• 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/5201266
• 关键词: carboxylate; chelating agents; chemical binding; chemical kinetics; chemical stability; chemical substitution; chemical synthesis; diagnostic tests; ligands; 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 novel acyclic ligand was required. Information acquired from evaluation of the solution chemistry of this compound, the kinetic and thermodynamic properties, and the serum stability has 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 terminated at the end of 1995 and the information gained will be transferred to project number Z01 CM 06399-04 RO.

该项目的主要目标是了解 聚氨基羧酸盐配体的基本配位化学 其中一种或多种羧酸盐被酚盐金属取代 结合位点。 因此，需要合成一种新型无环配体。 从溶液化学评估中获得的信息 化合物、动力学和热力学性质以及血清 稳定性已被用来衡量潜在的有用性 体内复合物。 这些研究为双功能的合理设计提供了基础。 用于络合用作杀细胞剂或诊断剂的金属的配体。 上述研究结果表明，就其本身而言， 邻羟基苄基金属结合位点，当掺入 聚氨基羧酸酯配体，不能提供足够稳定的复合物 体内。 然而，从综合中获得的知识提供了 类似苯硫酚类配体的合理合成路线 因此，该项目将于 1995 年底终止， 获得的信息将转移到项目编号 Z01 CM 06399-04 罗。