Inhibition of avian myeloblastosis virus reverse transcriptase by heterocyclic quinones: structure-activity correlation.
Synthetic heterocyclic quinones (107 samples) consisting of o- and p-quinoline quinones, o-isoquinoline quinones and p-quinoxaline quinones as well as o- and p-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, o-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 o-quinoline quinones. The longer the chain length of 7-alkyl substituent in o- or p-quinoline quinones, the lower the biological activities.
Inouye
Y
Y
Institute of Pharmaceutical Sciences, Hiroshima University School of Medicine, Japan.
Matsumoto
H
H
Morishige
R
R
Kitahara
Y
Y
Kubo
A
A
Nakamura
S
S
D009189:Avian Myeloblastosis Virus / Q000201:enzymology*; D011809:Quinones / Q000494:pharmacology*; D018894:Reverse Transcriptase Inhibitors; D013329:Structure-Activity Relationship
D011809:Quinones; D018894:Reverse Transcriptase Inhibitors