Substitution at the F-Ring N-Imide of the Indolocarbazole Antitumor Drug NB-506 Increases the Cytotoxicity, DNA Binding, and Topoisomerase I Inhibition Activities

The antitumor drug NB-506, which is currently undergoing phase I/II clinical trials, contains a DNA-intercalating indolocarbazole chromophore substituted with a glucose residue. In addition to interacting with DNA, the drug stabilizes the topoisomerase I−DNA covalent complex. To reinforce the DNA bi...

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Veröffentlicht in:	Journal of medicinal chemistry 1999-07, Vol.42 (15), p.2927-2935
Hauptverfasser:	Bailly, Christian, Qu, Xiaogang, Chaires, Jonathan B, Colson, Pierre, Houssier, Claude, Ohkubo, Mitsuru, Nishimura, Susumu, Yoshinari, Tomoko
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - metabolism Antineoplastic Agents - pharmacology Biological and medical sciences Carbazoles - chemical synthesis Carbazoles - chemistry Carbazoles - metabolism Carbazoles - pharmacology Cattle Circular Dichroism DNA - metabolism DNA, Neoplasm - metabolism Drug Screening Assays, Antitumor Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - metabolism Enzyme Inhibitors - pharmacology General aspects Glucosides - chemical synthesis Glucosides - chemistry Glucosides - metabolism Glucosides - pharmacology Humans indolocarbazole Inhibitory Concentration 50 Intercalating Agents - chemical synthesis Intercalating Agents - chemistry Intercalating Agents - metabolism Intercalating Agents - pharmacology Medical sciences NB-506 Pharmacology. Drug treatments Sequence Analysis, DNA Spectrometry, Fluorescence Spectrophotometry, Ultraviolet Structure-Activity Relationship Topoisomerase I Inhibitors Tumor Cells, Cultured
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