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Title: Non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 11: Structural modulations of diaryltriazines with potent anti-HIV activity
Authors: Xiong, Yuan-Zhen ×
Chen, Fen-Er
Balzarini, Jan
De Clercq, Erik
Pannecouque, Christophe #
Issue Date: Jun-2008
Series Title: European Journal of Medicinal Chemistry vol:43 issue:6 pages:1230-1236
Abstract: A series of novel 6-naphthyloxy substituted DATA analogues bearing different substituents on the C-6 position of triazine ring were synthesized and evaluated for their in vitro anti-HIV activity in MT-4 cells. The results demonstrated that most of the compounds in this series are potent activity against HIV-1 with moderate to high selectivity. Among these analogues, two compounds exhibited excellent effect in inhibiting HIV-1 replication at nanomolar concentration (for compound 9h: IC(50)=9.3nM, SI=15,385; for compound 9i: IC(50)=9.4nM, SI=14,094), which are about 15-fold more active than nevirapine. In addition, several compounds are active against both HIV-1 and HIV-2, whose mechanism may be different from typical NNRTIs.
URI: 
ISSN: 0223-5234
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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