B-Decachloro-o-carborane Derivatives suitable for the preparation of boron-labeled biological macromolecules.
B-decachloro-o-carborane derivatives in which one of the carbon atoms was substituted by -CH2CH2CO2H (I), -CH2CHOHCH2-O-CH2CH=CH2 (II) and -CH2CHOHCH2-O-p-C6H4NHCOOC(CH3)3 (III) were prepared from decachloro-o-carborane and the corresponding bromo (I) or epoxi (II and III) derivatives under alkaline conditions. II could be epoxidized and bound to dextran, Concanavalin A, and human IgG, with a boron content of 4.3, 4.8, and 4.9% (w/w), respectively. III could be converted to the corresponding amine and further to the isothiocyanate. Such boron derivatives could be suitable compounds for neutron capture therapy of tumors, as they are well water soluble and could be attached to tumor specific antibodies.
D001880:Boranes; D001895:Boron / Q000627:therapeutic use*; D001896:Boron Compounds; D055598:Chemical Phenomena; D002621:Chemistry; D006801:Humans; D009369:Neoplasms / Q000532:radiotherapy*; D009502:Neutrons; D011868:Radioisotopes / Q000627:therapeutic use*; D000098851:Carboranes
D001880:Boranes; D001895:Boron; D001896:Boron Compounds; D011868:Radioisotopes; C036367:B-decachloro-1,2-dicarbadecaborane; D000098851:Carboranes