Title: Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors
Authors: Yan, Zi-Hong ×
Wu, Hai-Qiu
Chen, Wen-Xue
Wu, Yan
Piao, Hu-Ri
He, Qiu-Qin
Chen, Fen-Er
De Clercq, Erik
Pannecouque, Christophe #
Issue Date: Jun-2014
Series Title: Bioorganic & medicinal chemistry vol:22 issue:12 pages:3220-6
Article number: 10.1016/j.bmc.2014.03.020
Abstract: A series of new diarylpyrimidines (DAPYs) characterized by a halogen atom on the methylene linker between wing I and the central pyrimidine ring was synthesized and evaluated for their anti-HIV activity in MT-4 cell cultures. The two most promising compounds 7f and 7g showed excellent activity against wild-type HIV-1 with low nanomolar EC50 values of 0.005 and 0.009 μM, respectively, which were comparable to or more potent than all the reference drugs zidovudine (AZT), lamivudine (3TC), nevirapine (NEV), efavirenz (EFV), delaviridine (DLV) and etravirine (ETV). In particular, 7g also displayed strong activity against the double mutant strain 103N + 181C with an EC50 value of 8.2 μM. The preliminary structure-activity relationship (SAR) and molecular docking analysis of this new series of CHX-DAPYs were also investigated.
ISSN: 0968-0896
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
Centre of Microbial and Plant Genetics
× corresponding author
# (joint) last author

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