Overview Oncologic, Endocrine & Metabolic: Oncologic, Endocrine & Metabolic :Ellipticine and related anticancer agents

Ellipticine (E), 9-methoxyellipticine (9ME) and olivacine are antitumour alkaloids isolated from Ochrosia elliptica and Aspidosperma olivaceum. 9-Hydroxyellipticine (9HE), a metabolite of 9ME, exhibits higher potency than E, but water insolubility has hampered its progression to clinical trials. A number of water soluble derivatives with, for example, a quaternary ammonium ion at position 2 or an amino-alkyl substituent at position 1, have been synthesised to overcome this problem. Elliptinium (2-methyl-9HE), datelliptium (2(diethylamino)ethyl-9HE), retelliptine (1-diethyl-aminopropy-lamino-9ME; BD-84), pazellipticine (1-diethyl-aminopropylamino-9-aza-OL; BD-40), elliprabin (2-arabinosyl-9HE), RPL-6 (carbamate at position 5 of E) and S-16020 (1-diethylaminoethylolivacine) have been extensively studied. Among these, elliptinium and datelliptium have been used for treatment of advanced breast cancer. Ellipticine analogues intercalate with DNA and show inhibition of topoisomerase II, as well as ditercalinium...

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