53 research outputs found
Inhibition of nucleoside and sugar transport into cells by an oncostatic methylase inhibitor, 5′-deoxy-5′-S-isobutyl-thioadenosine (SIBA)
Synthesis and biological activity of isogranulatimide analogues
The synthesis of new isogranulatimide analogues, their inhibitory activities toward the Checkpoint 1 kinase (Chk1), and their in vitro cytotoxicities toward four tumor cell lines (one murine L1210 leukemia, and three human cell lines: DU145 prostate carcinoma, A549 non-small cell lung carcinoma, and HT29 colon carcinoma) are described. The affinity for DNA of some representative compounds and their ability to induce DNA cleavage mediated by topoisomerase I have been examined. In some of the newly synthesized compounds, the imidazole heterocycle of isogranulatimide is replaced by a pyrrole and/or the indole unit is replaced by a 7-azaindole. Compounds in which a sugar part is attached to the 7-azaindole moiety have also been prepared. Some of the newly synthesized compounds are more potent Chk1 inhibitors than granulatimide. The selectivity of two potent Chk1 inhibitors 24 and 26 has been evaluated using various kinases. The strongest inhibitory properties are found toward Chk
Synthesis and cytotoxic activity of pyridazino[1 ',6 ': 1,2] pyrido[3,4-b]indol-5-inium derivatives as anti-cancer agents
Several new pyridazino[1′,6′:1,2]pyrido[3,4-b]indol-5-inium derivatives were synthesised from β-carboline derivatives and their cytotoxic activity and effect on the cell cycle were evaluated against L1210 cancer cells
Analogues of antifungal tjipanazoles from rebeccamycin
Analogues of antifungal tjipanazoles were obtained by semi-synthesis from rebeccamycin, an antitumor antibiotic isolated from cultures of Saccharothrix aerocolonigenes. The antiproliferative activities of the new compounds were evaluated in vitro against nine tumor cell lines. The effect on the cell cycle of murine leukemia L1210 cells was examined and the antimicrobial activities against two Gram positive bacteria, a Gram negative bacterium and a yeast were determined. The inhibitory properties toward four kinases and toward topoisomerase I were evaluated. The most cytotoxic compound in the series was a dinitro derivative characterized as a potent topoisomerase I inhibito
Nouveaux dérivés de [3,4-c]carbazole et de pyrido[2,3-b]pyrrolo[3,4-e]indole, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent
Synthesis and Biological Activity of Chimeric Structures Derived from the Cytotoxic Natural Compounds Dolastatin 10 and Dolastatin 15 †
Synthesis of New Aromatic Pyrrolo[2,1- c] [1,4]benzodiazepines and Pyrrolo[1,2- a] thieno[3,2- e] [1,4]diazepines as Anti-tumoral Agents
Nouveaux dérivés de [3,4-a:3,4-c]carbazole, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent
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