| Abstract
| - Three series of new boron-containing spermidine/spermine (SPD/SPM)analogues have beensynthesized: N- andN5-(4-carboranylbutyl) SPD/SPM derivatives(SPD-1, SPD-5, SPM-1,SPM-5);N1,N10-diethyl-N5-(4-carboranylbutyl)spermidine(DESPD-5),N1,N14-diethyl-N5-(4-carboranylbutyl)spermine (DESPM-5); andN5,N10-bis(4-carboranylbutyl)spermine(SPM-5,10).In vitro studies using rat F98 glioma cells have shown that thesepolyamines retain the abilityto displace ethidium bromide from calf thymus DNA and are rapidly takenup by F98 gliomacells. However, their cytotoxicities, especially those withterminal N-substituted (SPD-1, SPM-1) boron compounds, are greater than those of SPD/SPM.Nevertheless, the groundwork hasbeen created for a new class of boron-containing compounds that maybeuseful for boron neutroncapture therapy of tumors.
|
