Author/Authors :
Tetsuji Kawamoto، نويسنده , , Yoshihiro Ikeuchi، نويسنده , , Junko Hiraki، نويسنده , , Yoshiteru Eikyu، نويسنده , , Kazue Shimizu، نويسنده , , Masaki Tomishima، نويسنده , , Kiyoshi Bessho، نويسنده , , Fumio Yoneda، نويسنده , , Yuji Mikata، نويسنده , , Mamiko Nishida and، نويسنده , , Kenji Ikehara، نويسنده , , Takuma Sasaki، نويسنده ,
Abstract :
A series of nitro 5-deazaflavins, 5-deazaflavins possessing a nitro group at C(6)–C(9) position, has been designed and synthesized as a novel class of bioreductive nitrohetero-aromatic compounds and their cytotoxicities towards L1210 and KB cells were evaluated. It has been found that the nitro 5-deazaflavins undergo one electron reduction on the nitro group and undergo two electrons or “(net) hydride” reduction on the C(5)-C(4a)-C(10a)-N(1) redox system. They showed much more potent antitumor activities than the other 5-deazaflavins bearing no nitro group. These results suggest that an activation of nitro group by biological one electron reduction is crucial for an expression of cytotoxicity.