Synthesis of Bis‐acridine Derivatives Exhibiting Anticancer and Anti‐inflammatory Activity. (7th March 2013) - Sondhi, Sham M.
Abstract A series of bis‐acridine derivatives 3a–j and 5a–j have been synthesized by condensation of 9‐chloro‐2, 4‐(un)substituted acridines (1a–e) and 9‐isothiocyanato‐2, 4‐(un)substituted acridines (4a–e) with diamine 2a and 2b, respectively. These bis‐acridines were evaluated in vitro for activity against a panel of human cancer cell lines of lung (NCI H‐522), ovary (PA1), breast (T47D), colon (HCT‐15), and liver (HepG2). Several bis‐acridines were found to possess good anticancer activity against various cancer cell lines. Of these, compound 3h exhibited good anticancer activity against all cancer cell lines tested except liver (HepG2) cell line. In addition to this, these compounds were screened for anti‐inflammatory activity at a dose of 50 mg/kg p.o. Compound 3g exhibited 41% 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.