Design, Synthesis and Anticancer Evaluation of Carbazole Fused Aminopyrimidine Derivatives

Carbazole is an important type of tricyclic nitrogen containing compound and isolated first from coal tar in 1872 by Graebe and Glazer. Carbazole alkaloids have received considerable attention since their discovery in the 1960’s and their derivatives are well known for their pharmacological activities. Many recent studies have reported that carbazole derivatives exhibit a variety of biological activities. Toxicity of test compound in cells was determined by MTT assay based on mitochondrial reduction of yellow MTT tetrazolium dye to a highly blue colored formazan product. Among the ten synthesized compounds, 12c, 12d, 12e, 12f, 12g and 12i were showed good activity. In which 12c, 12d and 12e showed moderate activity on MCF-7 cancer cell line. Compounds 12f, 12g and 12i showed more potent activity than control. Compounds 12f, 12g and 12i showed more potent activity than control adriamycin. In future, we will plan further mechanistic studies on most potent active compounds 12f, 12g and 12i.