Messaoudi Samir, Anizon Fabrice, Léonce Stéphane, Pierré Alain, Pfeiffer Bruno, Prudhomme Michelle
Université Blaise Pascal, Synthèse et Etude de Systèmes à Intérêt Biologique, UMR 6504 du CNRS, 63177 Aubière, France.
Eur J Med Chem. 2005 Oct;40(10):961-71. doi: 10.1016/j.ejmech.2005.04.002.
The synthesis of a family of rebeccamycin analogues in which one indole unit has been replaced by a 7-azaindole moiety is described.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.
描述了一类瑞贝克霉素类似物的合成，其中一个吲哚单元已被7-氮杂吲哚部分取代。已在酰亚胺氮、咔唑骨架和糖部分进行了取代。还制备了具有内酰胺上杂环的化合物。评估了新合成化合物对四种肿瘤细胞系的细胞毒性，一种小鼠白血病（L1210）和三种人类肿瘤细胞系（前列腺癌DU145、结肠癌HT29和非小细胞肺癌A549），并与瑞贝克霉素以及母体非氮杂和氮杂化合物的细胞毒性进行了比较。
