COMPETITIVE FLUORESCENCE POLARIZATION STUDY OF THE BINDING OF 1,4-DIHYDROXY-5,8-BIS[[2-[(2-HYDROXYETHYL)AMINO]ETHYL]AMINO]9-10-ANTHRACENEDIONE TO DNA

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  • 1 January 1980
    • journal article
    • research article
    • Vol. 27  (3) , 497-506
Abstract
1,4-Dihydroxy-5,8-bis[[2-[(2-hydroxyethyl)amino]ethyl]amino]9-10-anthracenedione is undergoing Phase I clinical trials as an experimental antitumor agent. Fluorescent polarization was used to determine the extent of inhibition of the binding of acridine orange to DNA. Displacement of 50% of the acridine orange was achieved by 0.21 .mu.M of the title compound, 0.32 .mu.M daunorubicin, 0.41 .mu.M doxorubicin, 0.61 .mu.M dactinomycin and 7.8 .mu.M cis-platinum. Binding inhibition was essentially equivalent with natural DNA (calf thymus and Micrococcus luteus) and synthetic polymers [poly d(A):d(T) and poly d(G):d(C)] of widely differing adenine plus thymidine content.