Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 40, Issue 10, Pages 961-971Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2005.04.002
Keywords
rebeccamycin; 7-azaindole; antitumor compounds; topoisomerase I inhibitors
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The synthesis of a family of rebeccamycin analogues in which one indole unit has been replaced by a 7-azaindole moiety is described. Substitutions have been carried out on the imide nitrogen, on the carbazole framework and on the sugar part. Compounds with a lactam upper heterocycle have also been prepared. The cytotoxicities of the newly synthesized compounds toward four tumor cell lines, one murine leukemia (L1210) and three human tumor cell lines (prostate carcinoma DU145, colon carcinoma HT29, and non-small cell lung carcinoma A549) have been evaluated and compared to those of rebeccamycin and parent non-aza and aza compounds. (c) 2005 Elsevier SAS. All rights reserved.
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