ortho-Carboranyl Glycosides for the Treatment of Cancer by Boron Neutron Capture Therapy
| Autor: | Tietze, LF, Bothe, U, Griesbach, U, Nakaichi, M, Hasegawa, T, Nakamura, Hiroyuki, Yamamoto, Y |
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| Rok vydání: | 2001 |
| Předmět: |
Male
inorganic chemicals Stereochemistry Clinical Biochemistry Disaccharide Pharmaceutical Science chemistry.chemical_element Boron Neutron Capture Therapy 010402 general chemistry 01 natural sciences Biochemistry Chemical synthesis chemistry.chemical_compound Glucoside Drug Discovery Animals Glycosides Rats Wistar Boron Melanoma Molecular Biology chemistry.chemical_classification Aqueous solution Brain Neoplasms 010405 organic chemistry Organic Chemistry Radiochemistry Glycoside Biological activity Glioma Rats 0104 chemical sciences 3. Good health chemistry Molecular Medicine Carborane |
| Zdroj: | Bioorganic & Medicinal Chemistry. 9:1747-1752 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/s0968-0896(01)00061-x |
| Popis: | Distinct biological properties of the ortho-carboranyl (1,2-dicarba-closo-dodecaboranyl) glycosides 1, 2 and 3 were evaluated to estimate the suitability of these compounds for cancer treatment by boron neutron capture therapy. The boron uptake into B16-Melanoma cells was significantly higher by incubating the cells with aqueous solutions of carboranyl glucoside 1 (11.2 ppm after 3 h), lactoside 2 (13.2 ppm after 12 h) and maltoside 3 (20.0 ppm after 24 h) compared with solutions of clinically used p-boronophenylalanine (BPA) 5 (3.1 ppm after 24 h). Carboranyl maltoside 3 was more effective than boron-10 enriched 5 in killing C-6 rat glioma cells by incubating the cells 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 concentration of boron in the tumor tissue was 3.0 ppm. |
| Databáze: | OpenAIRE |
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