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（改编自应用程序）：硼中子捕获治疗 用于治疗癌症的BNCT已进入I期和II期临床试验。 多面体硼在正在进行的试验中占主导地位。 许多生物分子的多面体硼烷和碳硼烷衍生物，如氨基， 酸、核苷酸、核酸、卟啉、抗体等已经被 作为可能的下一代BNCT试剂。这些衍生品通常 基于B-10或B-12笼。一种新的[B_（22）H_（22）]_（2-）的简便合成 发现了NaBH_4（或富含B-10的NaBH_4）的多面体笼。 在结构上，它可以被认为是十硼烷（B10 H14）和 [B12 H12]2-笼，许多BNCT试剂的两种主要起始材料。 阶段I的具体目的是制备本发明化合物的碳硼烷基衍生物。 [B22 H22]2笼。用[B22 H22]2-的碳硼烷基衍生物取代 通常的B10或B12笼将立即使BNCT的生物分子成为可能 硼含量增加两倍。[B22 H22]2的另一种应用- 将其附着在DNA或肽探针上，用于一种新的专利技术， 诊断技术 拟议商业应用：不可用