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"Reverse" and "symmetrical" analogues of actinomycin D: metabolic activation and in vitro and in vivo tumor growth inhibitory activities.
Two new classes of actinomycin D analogues, tetracyclic "reverse" analogues and a tricyclic "symmetrical" analogue of actinomycin D, are reported. These analogues bind to DNA and the binding does notExpand
Preparative-scale high-performance liquid chromatographic separation and purification of 3'-azido-3'-deoxythymidine-5'-phosphate.
The practical and rapid preparative chromatographic method is being applied to the purification of AZT-P and other antiretroviral dideoxynucleotides, used as intermediates in the synthesis of target-directed experimental drugs for the treatment of AIDS. Expand
Potential radiosensitizing agents. Dinitroimidazoles.
New compounds of the nitroimidazole series have been synthesized as radiosensitizers which selectively sensitize hypoxic cells to the lethal effect of radiation. The reaction ofExpand
Hydroxymethylation and cyanoethylation of nitroimidazoles
A series of nitroimidazoles were subjected to hydroxymethylations under a variety of conditions. Hydroxymethylation of 1-(2-hydroxyethyl), 1-(2-acetoxyethyl), and 1-(2-chloroethyl) substitutedExpand
Potential radiosensitizing agents. 2. Synthesis and biological activity of derivatives of dinitroimidazole with oxiranes.
The results of radiosensitizing activity of these agents against hypoxic Chinese hamster cells (V-79) indicated that 2,4-dinitroimidazoles were better sensitizers than the nitroIMidazo[2,1-b]oxazoles, suggesting the necessity of the 2-nitro function in the molecule. Expand
Inhibitory effect of E-5-(2-bromovinyl)-1-beta-D-arabinofuranosyluracil on herpes simplex virus replication and DNA synthesis
BVaraU was a less effective antiherpesvirus agent than BVdUrd; unlike BVDUrd, it did not appear to be internally incorporated into replicating DNA in virus-infected cells. Expand
Lipid conjugates of antiretroviral agents. I. Azidothymidine-monophosphate-diglyceride: anti-HIV activity, physical properties, and interaction with plasma proteins.
3'-Azido-3'-deoxythymidine-5'-phosphate diglyceride (16:0/18:1 omega 9), a phosphatic acid conjugate of AZT, is active against HIV replication in H9 cells and syncytia formation in MOLT-3 cells. TheExpand
Enzymic and chemical reduction of 2-deaminoactinomycins to free radicals.
It is shown that actinomycin derivatives and their corresponding peptide-free diethylamino derivatives are more effective than the parent AMD in forming ion radicals, in stimulating oxygen uptake and in forming superoxide anion when incubated in the presence of NADPH and NADPH cytochrome P-450 reductase. Expand