Etude de la cytotoxicite in vitro de derives du carbazole III. 3-Amino et 3-nitro-1,4-dimethyl-9H-carbazoles diversement substitutes en position 6

Article abstract of DOI:10.1016/0223-5234(90)90197-B

The synthesis of a series of nitro and amino-1,4-dimethyl-9H-carbazoles is described.The cytotoxic activities, as assayed in vitro using clonogenic cell culture of murine leukemia L1210, vary greatly with the nature and position of substituents.The most cytotoxic derivatives, 3-amino-6-hydroxy 1,4-dimethyl-9H-carbazole, displays an activity similar to that of N2-methyl-9-hydroxy ellipticinium acetate (NMHE).These results, together with those previously published by us, allow a detailed analysis of structure-activity relationships in the 9H-carbazole and1,4-dimethyl-9H-carbazole series.For the 3-amino-1,4-dimethyl 9H-carbazole derivatives, a mechanism of action similar to that of ellipticine derivatives is proposed.