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.

提出的工作重点是含硼生物分子的合成和表征。这项研究的重要性在于所制备的分子可用于硼中子俘获治疗（BNCT）。虽然这项技术已经被人们知道了35年，但直到最近才被人们接受为治疗癌症的一种替代方法，比如脑肿瘤或多形性神经胶质瘤。由于血液到肿瘤的比率仍然相对较低，因此需要制备更多的选择性试剂用于该技术。靶向分子，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，应该提高这些化合物的选择性，并导致使用BNCT更有效的治疗。因此，提出的工作的主要具体目的是研究导致制备这类化合物的合成途径。如果在制备这些类型的化合物方面取得成果，生物医学领域对癌症研究的影响可能是惊人的。除了使用其他更传统的化疗技术外，BNCT的使用可以将这种方法用于脑肿瘤和胶质瘤以外的其他类型的癌症。用于制备这些化合物的合成技术将在首席研究员的研究实验室中开发，并且在某些情况下，将基于对氢化硼化学中使用的已知合成程序的改编。所制备化合物的表征将通过核磁共振（NMR）光谱、红外光谱、元素分析、质谱以及可能时合成化合物的单晶x射线晶体学来实现。在这些化合物的化学方面获得的知识将有助于促进对制备这些化合物家族所需的反应条件的理解，并可能导致BNCT作为癌症治疗的替代或补充方法的广泛适用性。