A new series of potential DNA bisintercalators have been designed by linking 8-hydroxy-quinoline to the 6-CH(2)OH group of glucose and connecting the 1-OH group of glucose with various linkers, such as quinol, glycol, and triethylene glycol. These new compounds were well-synthesized and fully characterized. Preliminary binding assays of these compounds to calf thymus DNA (CT-DNA) were conducted using UV-absorption and fluorescence spectroscopy analysis. The primary antitumor activity of these compounds was also performed.