Synthesis/ Characterization of Boronated Biomolecules

硼化生物分子的合成/表征

• 批准号: 6469252
• 负责人: William Quintana
• 金额: $ 6.87万
• 依托单位: NEW MEXICO STATE UNIVERSITY LAS CRUCES
• 依托单位国家: 美国
• 财政年份: 2001
• 资助国家: 美国
• 起止时间: 2001-06-01 至 2002-05-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6469252
• 关键词: X ray crystallography; boranes; boron; chemical structure function; chemical synthesis; drug design /synthesis /production; infrared spectrometry; mass spectrometry; neutron radiation; nuclear magnetic resonance spectroscopy

The emphasis of the proposed work is the synthesis and characterization of boron containing biomolecules. The importance of the research proposed stems from the fact that the molecules prepared could be used in boron neutron capture therapy (BNCT). This technique, although known for over 35 years, it is only recently gaining acceptance as an alternative method for the treatment of cancer, such as brain tumors or gliomas multiforme. There is a need for the preparation of more selective reagents for use in this technique, since the blood to tumor ration is still relatively low. Targeting molecules, such as amino acids, peptides, hormones and other regulatory molecules as components of the boronated unit, should enhance the selectivity of these compounds and result in a more efficient treatment using BNCT. Therefore, the main specific aim of the proposed work is the study of synthetic pathways leading to the preparation of this type of compounds. The implications of the biomedical field in cancer research can be staggering if the proposed results in the preparation of these types of compounds. The use of BNCT, in addition to other more traditional chemotherapeutical techniques can result in advancement of this approach to other types of cancer, besides brain tumors and gliomas. The synthetic techniques that will be employed to achieve the preparation of these compounds will be developed in the principal investigator's research laboratory and will be based, on some cases, on adaptations of known synthetic procedures use in boron hydride chemistry. Characterization of the prepared compounds will be achieved by using nuclear magnetic resonance (NMR) spectroscopy, Infrared spectroscopy, elemental analysis, mass spectrometry and when possible, single crystal X-ray crystallography of the synthesized compounds. The knowledge gained in the chemistry of these compounds will help advance the understanding of reaction conditions necessary for the preparation of these family of compounds and can result in the broad applicability of BNCT as an alternative or complimentary method in cancer treatment.

所提出的工作的重点是含硼的生物分子的合成和表征。该研究的重要性源于以下事实：制备的分子可以用于硼中子捕获疗法（BNCT）。该技术虽然已有35年以上的知名度，但它直到最近才被接受为治疗癌症的替代方法，例如脑肿瘤或多形胶质瘤。需要制备更多选择性试剂，以便在该技术中使用，因为血液到肿瘤的评分仍然相对较低。靶向分子，例如氨基酸，肽，激素和其他调节分子作为硼化单元的组成部分，应提高这些化合物的选择性，并使用BNCT进行更有效的处理。因此，提出的工作的主要特定目的是研究合成途径，从而制备这种类型的化合物。如果提出的化合物制备了拟议的化合物，则生物医学领域在癌症研究中的含义可能会令人震惊。除了其他更传统的化学治疗技术外，BNCT的使用还可能导致这种方法发展到其他类型的癌症，除了脑肿瘤和神经胶质瘤。主要研究者的研究实验室将开发用于实现这些化合物制备的合成技术，并基于某些情况，基于硼氢化氢化学中已知的合成程序的适应。通过使用核磁共振（NMR）光谱，红外光谱，元素分析，质谱法以及可能的情况下，将实现制备化合物的表征，并在合成化合物的单晶X射线晶体学上进行。这些化合物的化学知识将有助于促进对这些化合物家族制备所需的反应条件的理解，并可能导致BNCT作为癌症治疗中的替代或免费方法的广泛适用性。