Synthesis, anti-inflammatory and anticancer activity evaluation of some novel acridine derivatives

Condensation of 9-chloro-2,4-(un)substituted acridines (1a–c) with various amines (2a–e) and 9-isothiocyanato-2,4-(un)substituted acridines (4a,b) with different amines (2a,b,d,e) gave condensed products 3a–o and 5a–g respectively. Compounds 3a–o and 5a–g were screened for anti-inflammatory activity at a dose of 50 mg/kg p.o. Compound 3e exhibited 41.17% anti-inflammatory activity which is better than most commonly used standard drug ibuprofen which showed 39% anti-inflammatory (at 50 mg/kg p.o.) activity. Anticancer activity evaluation of compounds 3a–o and 5a–g was carried out against a small panel of human cancer cell lines and compounds 3g, 3m and 5g exhibited good anticancer activity against breast (MCF-7), liver (HEP-2), colon (COLO-205, 502713, HCT-15), lung (A-549) and neuroblastoma (IMR-32) cancer cell lines at a concentration of 1 × 10−5 M.

Graphical abstractSeveral acridine derivatives were synthesized and evaluated for anti-inflammatory and anticancer activities. Compound 3e exhibited very good anti-inflammatory activity and compounds 3g & 3m showed good anticancer activity .Figure optionsDownload full-size imageDownload as PowerPoint slide