Inhibition of Avian Myeloblastosis Virus Reverse Transcriptase by Heterocyclic Quinones: Structure-Activity Correlation

Abstract

Synthetic heterocyclic quinones (107 samples) consisting of o- and p-quinoline quinones, o-isoquinoline quinones and /7-quinoxaline quinones as well as o- and /7-naphthoquinones (3 samples) were tested for their inhibitory activities against avian myeloblastosis virus reverse transcriptase (AMV-RT) and cytotoxic activities against mouse lymphoblastoma L5178Y cells. In general, 0-quinoline quinones (i.e., the 5,6-quinolinedione derivatives) are more potent inhibitors of AMV-RT than p-quinoline quinones (the 5,8-quinolinedione derivatives). Furthermore, the growth of L5178/Y cells were significantly refractory to the 8-methoxy-5,6-quinolinedione derivatives whose suppressive effects on AMV-RT function were fairly comparable to those of the other 0-quinoline quinones. The longer the chain length of 7-alkyl substituent in 0- or p-quinoline quinones, the lower the biological activities. © 1991, The Pharmaceutical Society of Japan. All rights reserved.