ortho-Carboranyl glycosides for the treatment of cancer by boron neutron capture therapy

Distinct biological properties of the ortho-carboranyl (1,2-dicarba-closo-d odecaboranyl) glycosides 1, 2 and 3 were evaluated to estimate the suitabil ity of these compounds for cancer treatment by boron neutron capture therap y. The boron uptake into B16-Melanoma cells was significantly higher by inc ubating the cells with aqueous solutions of carboranyl glucoside 1 (11.2 pp m after 3 h), lactoside 2 (13.2 ppm after 12 h) and maltoside 3 (20.0 ppm a fter 24 h) compared with solutions of clinically used p-boronophenylalanine (BPA) 5 (3.1 ppm after 34 h), Carboranyl maltoside 3 was more effective th an boron-10 enriched 5 in killing C-6 rat glioma cells by incubating the ce lls with the compound and subsequent treatment with thermal neutrons. 3 was also administrated iv, in concentrations of 25 mg boron/kg body weight to rats bearing brain tumors. After a period of 4 h after administration the c oncentration of boron in the tumor tissue was 3.0 ppm. (C) 2001 Elsevier Sc ience Ltd. All rights reserved.