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The chemistry of antitumor antibiotics
Streptozocin. Pyrrolo (1,4) Benzodiazepines. Saframycins, Renieramycins, and Safracins. Naphthyridinomycin, Cyanocyclines, and Quinocarcin. CC-1065. Nogalamycin and Related Compounds. Streptonigrin
6- and 7-substituted 2-[2'-(dimethylamino)ethyl]-1,2-dihydro-3H-dibenz[de,h] isoquinoline-1,3-diones: synthesis, nucleophilic displacements, antitumor activity, and quantitative structure-activity
Ten of the new compounds were more potent than the unsubstituted compound, azonafide, in a panel of tumor cells including human melanoma and ovarian cancer and murine sensitive and MDR L1210 leukemia and one of them, 6-ethoxyazonafides, was nearly as potent against solid tumor cells as leukemia cells.
Amino-substituted 2-[2'-(dimethylamino)ethyl]-1,2-dihydro-3H- dibenz[de,h]isoquinoline-1,3-diones. Synthesis, antitumor activity, and quantitative structure--activity relationship.
Sets of 2-[2-(dimethylamino)ethyl]-1,2-dihydro-3H- dibenz[de,h]isoquinoline-1,3-diones with amino and actylamino groups at each of the eight positions on the anthracene nucleus were synthesized from
Analogues of amonafide and azonafide with novel ring systems.
Three new types of amonafide and azonafide analogues were synthesized and screened in a panel of human solid tumor cells and murine L1210 leukemia cells, and the phenanthrene and azaphenanthrene analogues showed no improvement on the potencies of the anthracenes.
Preclinical antitumor activity of the azonafide series of anthracene-based DNA intercalators
The results demonstrate that the 6-ethoxy substituted azonafide, AMP-53, has consistent (in vitro and in vivo) experimental antitumor activity in human breast and lung cancer, and could be considered for clinical testing in patients with MDR tumors.
Computer simulation of the binding of quinocarcin to DNA. Prediction of mode of action and absolute configuration
Computer-based models were derived for the covalent and noncovalent binding of the antitumor antibiotic quinocarcin to a representative DNA segment, d(ATGCAT)2 and showed that a mode of action, involving opening of the oxazolidine ring to give an iminium ion, was rational and attended by favorable interaction energies in each step.
Structure-activity comparison of mitomycin C and mitomycin A analogues (review).
Any MMA derivative would have a high likelihood of being more potent than its MMC equivalent but that its antitumor effects must be independently determined since they cannot be predicted from the results with MMC analogs.
1,4-disubstituted anthracene antitumor agents.
Although the 1,4-hydrazone was active against P388 leukemia in mice, it was inactive against L1210 leukemia and within each pair of compounds, the one with greater average potency against tumor cells gave a greater increase in the transition melt temperature of DNA.