Ellipticine analogues and related compounds as inhibitors of reverse transcriptase and as inhibitors of the efflux pump

Ten polycyclic derivatives related to ellipticine have been synthesised and tested for their intercalating, reverse transcriptase (RT) inhibitory and multidrug resistance eff lux pump inhibitory properties, The intercalating activity and the RT inhibitory activity of the derivatives suggest that ell ipticine analogues bind at an allosteric binding site on RT or that this in hibition could be controlled at the DNA level. The MDR eff lux pump inhibit ory activities of these derivatives, however, appears to be unrelated to th e DNA binding ability.