Simplified catechin-gallate inhibitors of HIV-1 reverse transcriptase.
Systematic simplification of the molecular structures of epicatechin gallate and epigallocatechin gallate to determine the minimum structural characteristics necessary for HIV-1 reverse transcriptase inhibition in vitro resulted in several compounds that strongly inhibited the native as well as the A17 double mutant (K103N Y181C) enzyme, which is normally insensitive to most known nonnucleoside inhibitors.
Tillekeratne
L M
LM
Department of Medicinal and Biological Chemistry, College of Pharmacy, University of Toledo, Toledo, OH 43606, USA.
Sherette
A
A
Grossman
P
P
Hupe
L
L
Hupe
D
D
Hudson
R A
RA
D002392:Catechin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000235:genetics; D009154:Mutation; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D018894:Reverse Transcriptase Inhibitors; C417939:catechin gallate; D002392:Catechin; C062669:epicatechin gallate; C045651:epigallocatechin gallate; D054303:HIV Reverse Transcriptase