Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
A novel oxindole was discovered as an HIV non-nucleoside reverse transcriptase inhibitor via HTS using a cell-based assay. Systematic structural modifications were carried out to establish its SAR. These modifications led to the identification of oxindoles with low nanomolar potency for inhibiting HIV replication. These novel and potent oxindoles could serve as advanced leads for further optimizations.
Jiang
Tao
T
Genomics Institute of the Novartis Research Foundation (GNF), 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA.
Kuhen
Kelli L
KL
Wolff
Karen
K
Yin
Hong
H
Bieza
Kimberly
K
Caldwell
Jeremy
J
Bursulaya
Badry
B
Wu
Tom Yao-Hsing
TY
He
Yun
Y
D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000494:pharmacology; D024882:Drug Resistance, Viral; D015497:HIV-1 / Q000187:drug effects*; D007211:Indoles / Q000138:chemical synthesis / Q000494:pharmacology; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014779:Virus Replication
D019380:Anti-HIV Agents; D007211:Indoles; D018894:Reverse Transcriptase Inhibitors