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Boron Clusters with 10B Isotope

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Boron Clusters with 10B Isotope for Boron Neutron Capture Therapy of Cancer (BNCT)

Tech Area / Field

  • CHE-SYN/Basic and Synthetic Chemistry/Chemistry
  • MED-RAD/Radiomedicine/Medicine

Status
3 Approved without Funding

Registration date
10.07.2012

Leading Institute
Tbilisi State University, Georgia, Tbilisi

Collaborators

  • Northern Illinois University, USA, Dekalb\nInstitute for Neutron Therapy (NIU), USA, IL, Batavia

Project summary

Research Objectives.
The present project is aimed to create a series of 10B-containing amino acids and peptides as potential agents for boron neutron capture therapy (BNCT) for cancer treatment. This objective can be pided into sub-objectives as detailed below:
1. Development of high-yield methods of synthesis for polyhedral boron hydrides from commercially available 10B-enriched material. This sub-objective includes
a) development of high-yield method for the synthesis of 10B-enriched sodium borohydride Na10BH4 from 10B-enriched boric anhydride 10B2O3;
b) development of high-yield methods for the synthesis of 10B-enriched closo-dodecaborate [10B12H12]2- and carba-closo-dodecaborate [C10B11H12]- from Na10BH4.
2. The investigation of methods of synthesis for amino acids and peptides incorporating the 10B-enriched closo-dodecaborate [10B12H12]2- and carba-closo-dodecaborate [C10B11H12]-.
3. Study of the resulting boronated amino acids and peptides in vitro and in vivo as potential agents for BNCT.
Thus, a series of novel boronated amino acids and peptides will be investigated and their properties as potential agents for BNCT will be evaluated.
Participants of the Project.
Two teams will be participating in this project.
The first group has the resources of 10B-enriched compounds and the experience in working with them.
The second team under the leadership of Professor Vladimir Bregadze has the experience in synthesizing the polyhedral borane derivatives for BNCT evaluation. The participants of the project have developed new methods of preparation for a variety of derivatives of closo-dodecaborate.
Expected Results and Their Application. The high-yield methods for the synthesis of 10B-enriched sodium borohydride, closo-dodecaborate and carba-closo-dodecaborate from commercially available 10B-enriched starting materials will be investigated. Methods of synthesis for novel boron-containing amino acids and peptides involving closo-dodecaborate and carba-closo-dodecaborate anions will be developed and a series of such compounds will be synthesized. The biochemical behavior of the compounds prepared for in vitro and in vivo tests will be investigated and their applicability as BNCT agents will be evaluated.
Meeting ISTC Goals and Objectives. The project will fulfill the objectives of ISTC in the following way: providing weapons scientists and engineers opportunities to redirect their talents to peaceful activities; promoting integration of scientists into the international scientific community; supporting basic and applied research and technology development for peaceful purposes; reinforcing the transition to market-based economics responsive to civil needs.
Scope of Activities. The investigation of high-yield methods of synthesis for 10B-enriched sodium borohydride from commercially available materials.
The investigation of high-yield methods of synthesis for 10B-enriched closo-dodecaborates and carba-closo-dodecaborates from Na10BH4.
The investigation of synthetic methods for preparation of boron-containing amino acids and peptides based on 10B-enriched closo-dodecaborates and carba-closo-dodecaborates and further evaluation of their applicability as BNCT drugs.
Role of Foreign Collaborators
- Information exchange during the execution of the Project;
- Carrying out joint experiments and investigation of complexes synthesized, if necessary;
- Discussions of obtained experimental results;
- Joint publications;
- Offering of conclusions on Technical Reports (quarterly, annual, and final) submitted to ISTC by Project executors;
- Conducting some experiments at the laboratories of Western collaborators.
Technical Approach and Methodology. Methods developed earlier will be applied and adapted for the synthesis of 10B-enriched sodium borohydride. The method based on the mild oxidation of sodium borohydride with iodine followed by pyrolysis [A.V.Geis, K.Guttsche, C.Knapp, H.Scherer, R.Uzun, Dalton Trans., 2009, 2687] will be applied and adapted for synthesis of 10B-enriched closo-dodecaborate. The method based on the oxidation of sodium borohydride with iodine followed by the mild pyrolysis and an insertion of carbon vertex will be applied and adapted for synthesis of 10B-enriched carba-closo-dodecaborate. The approach developed by the authors, based on the ring-opening of cyclic oxonium derivatives of polyhedral boron hydrides [A.A.Semioshkin, I.B.Sivaev, V.I.Bregadze. Cyclic Oxonium Derivatives of Polyhedral Boron Hydrides and Their Synthetic Applications. Dalton Transaction, 2008, 977-982], will be used for the synthesis of amino acids and peptides involving closo-dodecaborate. The standard approach based on the lithiation and alkylation of carboranes will be used for synthesis of amino acids incorporating carba-closo-dodecaborate. The compounds synthesized in this project will be characterized by the methods of multinuclear NMR and IR spectroscopy and X-ray diffraction analysis.


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The International Science and Technology Center (ISTC) is an intergovernmental organization connecting scientists from Kazakhstan, Armenia, Tajikistan, Kyrgyzstan, and Georgia with their peers and research organizations in the EU, Japan, Republic of Korea, Norway and the United States.

 

ISTC facilitates international science projects and assists the global scientific and business community to source and engage with CIS and Georgian institutes that develop or possess an excellence of scientific know-how.

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