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Title: Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors
Authors: Yan, Zi-Hong ×
Huang, Xia-Yun
Wu, Hai-Qiu
Chen, Wen-Xue
He, Qiu-Qin
Chen, Fen-Er
De Clercq, Erik
Pannecouque, Christophe #
Issue Date: Apr-2014
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:22 issue:8 pages:2535-41
Article number: 10.1016/j.bmc.2014.02.030
Abstract: A series of CR2(OH)-diarylpyrimidine derivatives (CR2(OH)-DAPYs) featuring a hydrophobic group at CH(OH) linker between wing I and the central pyrimidine were synthesized and evaluated for their anti-HIV activity in MT-4 cell cultures. All the target compounds except for compound 3k displayed inhibitory activity against HIV-1 wild-type with EC50 values ranging from 7.21±1.99 to 0.067±0.006μM. Among them, compound 3d showed the most potent anti-HIV-1 activity (EC50=0.067±0.006μM, SI>592), which was approximately 2-fold more potent than the reference drugs nevirapine (NVP) and delaviridine (DLV) in the same assay. In addition, the binding modes with HIV-1 RT and the preliminary SAR studies of these new derivatives were also investigated.
URI: 
ISSN: 0968-0896
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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