Synthesis and biological evaluation of new 9-aminoacridine-4-carboxamide derivatives as anticancer agents

The design of molecules that recognize the specific sequence of the DNA double helix or those that can stabilize DNA topoisomerase cleavable complex to stop the progression of DNA process, may be very useful in cancer chemotherapy. In the field of antituor DNA-intercalating agents, 9-aminoacridine-4-carboxamide derivatives play an important role due to their anti-proliferative properties. In the present study, 9-aminoacridine-4-carboxamide derivatives were designed, synthesized, characterized and evaluated against lung cancer (A-549) cell line and cervical cancer (HeLa) cell line in vitro by MTT assay. Compounds 5a, 5b and 5e were selected for anticancer evaluation against the lung cancer cell line and cervical cancer cell line. Compound 5b showed the maximum activity against the cervical cancer (HeLa) cell line with CTC50 (47.50 mu g/ml) and compound 5e showed the maximum activity against the lung cancer (A-549) cell line with CTC50 (100 mu g/ml) among the tested compounds. The present study opens new vista for DNA intercalating anticancer compounds and their further in vivo investigation. (C) 2011 King Saud University. Production and hosting by Elsevier B.V. All rights reserved.