Synthesis, anti-inflammatory, and cytotoxicity evaluation of 9,10-dihydroanthracene-9,10-alpha,beta-succinimide and bis-succinimide derivatives

摘要

9,10-Dihydroanthracene-9,10-alpha,beta-succinimide derivatives 4a-e and bis-succinimide derivatives 6a-e have been synthesized by grinding 9,10-dihydroanthracene-9,10-alpha,beta-succinic anhydride 2 with various mono 3a-e and diamines 5a-e in quantitative yields. All the target compounds were fully characterized by spectrometric and spectroscopic means. Compounds 4a-e, 6a-e and recently reported compounds 4f-p were screened for anti-inflammatory and for cytotoxicity against five human cancer cell lines: T47D, NCI H-522, HCT-15, PA1, and HepG-2. Compounds 4e, 4i, 4j, and 4p exhibited good anti-inflammatory activity and compounds with interesting cytotoxic profile were 4c, 6e (T47D); 4e, 4o (NCI H-522); 4n (HCT-15); 4e, 4h, 4o (PA1); and 4a, 4e, 4f, 4i, 4o (HepG-2).