Potent radiosensitizing agents: 5-methylselenyl- and 5-phenylselenyl-methyl-2'-deoxyuridine.
This Letter describes the novel radiosensitizing agents based on nucleoside base modification. In addition to the known 5-phenylselenide derivative, 5-methylselenide modified thymidine, which has a van der Waals radius smaller than the phenyl group, was newly synthesized. The similar monomer activity of 5-methylselenide derivative under oxidation condition was confirmed by NMR experiments. The cytotoxicity tests and radiosensitizing experiments of both compounds were carried out using the H460 lung cancer cell line. Both the 5-phenylselenide and the 5-methylselenide derivatives showed a relatively low toxicity to the cells. However, in combination with γ-radiolysis, both exerted good radiosensitizing effects to the lung cancer cell lines in vitro. This result confirms that 5-methylselenide modified thymidine could be a useful candidate as a potential radiosensitizing agent in vivo.
Department of Chemistry, College of Natural Science, Kongju National University, 182 Shinkwan-dong, Gongju, Chungnam 314-701, Republic of Korea.
Ambadas B
AB
Rode
Byeong Mo
BM
Kim
Seon Hwa
SH
Park
In Seok
IS
Hong
Sung Hee
SH
Hong
D045744:Cell Line, Tumor; D003857:Deoxyuridine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity; D005720:Gamma Rays; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D016566:Organoselenium Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D010084:Oxidation-Reduction; D011838:Radiation-Sensitizing Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity
C558288:5-methylselenylmethyl-2'-deoxyuridine; C558289:5-phenylselenylmethyl-2'-deoxyuridine; D016566:Organoselenium Compounds; D011838:Radiation-Sensitizing Agents; D003857:Deoxyuridine