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Chemistry and biology of some low molecular weight boron compounds for Boron Neutron Capture Therapy

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Abstract

Boronated DNA targeting agents are especially attractive candidatesfor BNCT because they may deliver boron-10 tothe nuclei of tumor cells. Numerous boron-containing analogshave been synthesized and some have shown promisingresults in initial biological tests. One of themost challenging tasks in this special field ofresearch remains the finding of suitable targeting strategiesfor the selective delivery of boron rich DNA-intercalator/alkylatorto tumor cells. Synthetic and biological studies ofboron compounds suitable for DNA-binding are reviewed.The amino acid p-boronophenylalanine (BPA) is presently ofconsiderable clinical interest. Other boronated amino acids mightalso be candidates for BNCT either per se,as part of part of tumor-seeking peptides orconjugated to targeting macromolecules. A large number ofboronated L- and D-amino acids with varying liphophicilityand sterical requirements are now available for evaluation.Recent synthetic and biological studies of aromatic boronoaminoacids, carboranylamino acids and carboranyl amines are alsoreviewed.

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Authors and Affiliations

  1. Department of Organic Chemistry, Uppsala University, Sweden

    Stefan Sjöberg, Hadi Ghaneolhosseini, Jonas Malmquist, Charlotta Naeslund & Werner Tjarks

  2. Biomedical Radiation Science, Uppsala University, Sweden

    Jörgen Carlsson, Lars Gedda, Torbjörn Hartman & Pär Olsson

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  1. Stefan Sjöberg
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  2. Jörgen Carlsson
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Sjöberg, S., Carlsson, J., Ghaneolhosseini, H. et al. Chemistry and biology of some low molecular weight boron compounds for Boron Neutron Capture Therapy. J Neurooncol 33, 41–52 (1997). https://doi.org/10.1023/A:1005756929011

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