Title of article :
Synthesis, in vitro evaluation, and docking studies of novel chromone derivatives as HIV-1 protease inhibitor
Author/Authors :
Jiraporn Ungwitayatorn، نويسنده , , Jiraporn and Wiwat، نويسنده , , Chanpen and Samee، نويسنده , , Weerasak and Nunthanavanit، نويسنده , , Patcharawee and Phosrithong، نويسنده , , Narumol، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2011
Pages :
10
From page :
152
To page :
161
Abstract :
Novel chromone derivatives with a benzopyran-4-one scaffold have been prepared by the one-pot cyclization reaction. The in vitro inhibitory activity of these new compounds towards HIV-1 protease have been evaluated using stop time HPLC method as the preliminary screening. The most potent compound, 7,8-dihydroxy-2-(3′-trifluoromethyl phenyl)-3-(3″-trifluoromethylbenzoyl)chromone (32), showed IC50 = 0.34 μM. The molecular docking study supported results from experimental activity testing and also provided structure–activity relationship of this series.
Keywords :
chromone derivatives , HIV-1 protease inhibitor , molecular docking
Journal title :
Journal of Molecular Structure
Serial Year :
2011
Journal title :
Journal of Molecular Structure
Record number :
1968662
Link To Document :
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