Synthesis, in vitro evaluation, and docking studies of novel chromone derivatives as HIV-1 protease inhibitor

…, W Samee, P Nunthanavanit, N Phosrithong

Index: Ungwitayatorn, Jiraporn; Wiwat, Chanpen; Samee, Weerasak; Nunthanavanit, Patcharawee; Phosrithong, Narumol Journal of Molecular Structure, 2011 , vol. 1001, # 1-3 p. 152 - 161

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Citation Number: 23

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 ...