Chem. Pharm. Bull. 50(11) 1479—1483 (2002)

member of the pyridocarbazole family of alkaloids. It was first isolated from the bark and stem of Aspidosperma olivaceum and it has been found to possess similar antitumor activity as its 5,11-dimethyl isomer, ellipticine, and related compounds like 9-methoxyellipticine. As the main mechanism of these agents’ antineoplastic action, a stabilization of the “cleavable complex” which is formed between DNA and the enzyme, topoisomerase II, is generally accepted, although additional mechanisms have been discussed for some pyridocarbazoles, e.g. reactivation of the lost functionality of the p53 protein. Based on the naturally occurring lead compounds, numerous modifications of this system have been studied, leading to the development of drugs like elliptinium, datelliptium, retelliptine, or pazelliptine. More recently, the highly potent olivacine analog, S160202, has attracted considerable attention due to its apparent ability to circumvent P-glycoprotein-mediated multidrug resistance.