title: Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
abstract: A novel series of quinolones was discovered as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) using a structure-based approach. The lead quinolones exhibited single digit nanomolar potency in the HIV-1 replication assays. The preliminary SAR of these quinolones was also established via systematic structural modifications. These novel and potent quinolones could serve as advanced leads for further optimization.
authors.affiliation: Genomics Institute of the Novartis Research Foundation (GNF), San Diego, CA 92121, USA.
authors.forename: David
authors.initials: D
authors.lastname: Ellis
authors.forename: Kelli L
authors.initials: KL
authors.lastname: Kuhen
authors.forename: Beth
authors.initials: B
authors.lastname: Anaclerio
authors.forename: Baogen
authors.initials: B
authors.lastname: Wu
authors.forename: Karen
authors.initials: K
authors.lastname: Wolff
authors.forename: Hong
authors.initials: H
authors.lastname: Yin
authors.forename: Badry
authors.initials: B
authors.lastname: Bursulaya
authors.forename: Jeremy
authors.initials: J
authors.lastname: Caldwell
authors.forename: Donald
authors.initials: D
authors.lastname: Karanewsky
authors.forename: Yun
authors.initials: Y
authors.lastname: He
mesh_terms: D001665:Binding Sites; D024882:Drug Resistance, Viral; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors; D015497:HIV-1 / Q000378:metabolism; D008956:Models, Chemical; D008958:Models, Molecular; D009154:Mutation; D015363:Quinolones / Q000737:chemistry; D018894:Reverse Transcriptase Inhibitors / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014779:Virus Replication
chemical_list: D015363:Quinolones; D018894:Reverse Transcriptase Inhibitors; D054303:HIV Reverse Transcriptase