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 efflux pump inhibitory properties. The intercalating activity and the RT inhibitory activity of the derivatives suggest that ellipticine analogues bind at an allosteric binding site on RT or that this inhibition could be controlled at the DNA level. The MDR efflux pump inhibitory activities of these derivatives, however, appears to be unrelated to the DNA binding ability.
Sharples
D
D
University of Manchester, School of Pharmacy and Pharmaceutical Sciences, Oxford Road, Manchester, M13 9PL, UK.
Hajós
G
G
Riedl
Z
Z
Csányi
D
D
Molnár
J
J
Szabó
D
D
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018432:Drug Resistance, Multiple; D004611:Ellipticines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007364:Intercalating Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000972:Antineoplastic Agents, Phytogenic; D004611:Ellipticines; D007364:Intercalating Agents; D018894:Reverse Transcriptase Inhibitors