NEW (B22H22)2 FOR NEUTRON CAPTURE AND DIAGNOSTICS

用于中子捕获和诊断的新型 (B22H22)2

• 批准号: 2776444
• 负责人: BERNARD F SPIELVOGEL
• 金额: $ 10万
• 依托单位: BORON BIOLOGICALS, INC.
• 依托单位国家: 美国
• 财政年份: 1999
• 资助国家: 美国
• 起止时间: 1999-03-15 至 2000-03-14
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/2776444
• 关键词: boranes; boron; chemical synthesis; drug design /synthesis /production; neoplasm /cancer diagnosis; neutron radiation; nucleic acid probes; radionuclide therapy

DESCRIPTION (Adapted from the application): Boron Neutron Capture Therapy (BNCT) for treatment of cancer has entered Phase I & II clinical trials. Polyhedral boron hydrides figure predominantly in the ongoing trials. Many polyhedral borane and carboranyl derivatives of biomolecules such as amino acids, nucleotides, nucleic acids, porphyrins, antibodies, etc. have been prepared as possible next generation BNCT agents. Such derivatives are usually based upon B-10 or B-12 cages. A convenient synthesis of a novel [B22H22]2- polyhedral cage from NaBH4 (or B-10 enriched NaBH4) has been discovered. Structurally it may be considered a hybrid of decaborane (B10H14) and the [B12H12]2- cage, the two principal starting materials for many BNCT agents. The specific aim of Phase I is to prepare a carboranyl derivative of the [B22H22]2- cage. Substitution of a carboranyl derivative of [B22H22]2- for the usual B10 or B12 cage would immediately make possible biomolecules for BNCT with a two-fold increase in boron content. Another application for [B22H22]2- would be its attachment to DNA or peptide probes for use in a new patented diagnostic technique. PROPOSED COMMERCIAL APPLICATION: NOT AVAILABLE

描述（根据应用程序改编）：硼中子捕获疗法 （BNCT）用于癌症的治疗已进入I和II期临床试验。 在正在进行的试验中，多面体硼氢化物的数字主要是在进行的。 许多生物分子的多面体硼烷和碳素衍生物，例如氨基 酸，核苷酸，核酸，卟啉，抗体等 准备下一代BNCT代理。这样的衍生物通常是 基于B-10或B-12笼。小说[B22H22] 2-的方便合成 已经发现了来自NABH4（或B-10富集的NaBH4）的多面体笼。 从结构上讲，它可能被认为是脱骨剂（B10H14）和 [B12H12] 2-笼，这是许多BNCT代理的两种主要起始材料。 第一阶段的具体目的是准备一个碳氧化氢衍生物 [B22H22] 2-笼。替代[B22H22] 2-的carboranyl衍生物代替 通常的B10或B12笼将立即使BNCT的生物分子成为可能 硼含量增加了两倍。 [B22H22] 2-的另一个应用程序 将是其附着在新专利的DNA或肽探针上 诊断技术。 拟议的商业应用程序：不可用