Biological Evaluation of Dodecaborate-Containing L-Amino Acids for Boron Neutron Capture Therapy

Research Center of Boron Neutron Capture Therapy, Research Organization for the 21st Century, Osaka Prefecture University, 1-1 Gakuen-cho, Nakaku 599-8531, Sakai, Japan.
Journal of Medicinal Chemistry (Impact Factor: 5.48). 07/2012; 55(15):6980-4. DOI: 10.1021/jm300749q
Source: PubMed

ABSTRACT To develop a boron carrier for practical purposes, new boron-containing amino acids with an undecahydro-closo-dodecaboranylthio ([(10)B(12)H(11)S](2-)-) unit in the side chain of the α-amino acid have already been designed and synthesized. In the present paper, cytotoxicity, the incorporation amounts into tumor cells, and the tumor cell killing effects of these compounds were elucidated to evaluate their usefulness as boron carriers. Furthermore, the microdistribution of the amino acids in tumor cells was established.