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

✍ Scribed by Derek Sharples; György Hajós; Zsuzsanna Riedl; Dorottya Csányi; József Molnár; Diana Szabó

• Publisher: John Wiley and Sons
• Year: 2001
• Tongue: English
• Weight: 100 KB
• Volume: 334
• Category: Article
• ISSN: 0365-6233
• DOI: 10.1002/1521-4184(200109)334:8/9<269::aid-ardp269>3.0.co;2-#

✦ Synopsis

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.