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Title: Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action
Authors: Mao, Tian-Qi ×
He, Qiu-Qin
Wan, Zheng-Yong
Chen, Wen-Xue
Chen, Fen-Er
Tang, Gang-Feng
De Clercq, Erik
Daelemans, Dirk
Pannecouque, Christophe #
Issue Date: Jul-2015
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:23 issue:13 pages:3860-8
Article number: 10.1016/j.bmc.2015.03.037
Abstract: A molecular hybridization approach is a powerful tool in the design of new molecules with improved affinity and efficacy. In this context, a series of diarylpyrimidine-quinolone hybrids were synthesized and evaluated against both wt HIV-1 and mutant viral strains. The most active hybrid 5a displayed an EC50 value of 0.28±0.07μM against HIV-1 IIIB. A couple of enzyme-based assays clearly pinpoint a RT-targeted mechanism of action. Docking studies revealed that these hybrids could be well located in the NNIBP of HIV-1 RT despite the bulky and polar properties of a quinolone 3-carboxylic acid moiety in the molecules.
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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