Design and discovery of flavonoid-based HIV-1 integrase inhibitors targeting both the active site and the interaction with LEDGF/p75

Bioorganic and Medicinal Chemistry

Volumn 22, Issue 12, 2014, Pages 3146-3158

  Li, Bo Wen ^a,b   Zhang, Feng Hua ^b   Serrao, Erik ^c   Chen, Huan ^d   Sanchez, Tino W ^c   Yang, Liu Meng ^d   Neamati, Nouri ^c   Zheng, Yong Tang ^d   Wang, Hui ^a   Long, Ya Qiu ^b  

^a SOUTH CHINA NORMAL UNIVERSITY   (China)

^b SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

^c UNIVERSITY OF SOUTHERN CALIFORNIA   (United States)

^d KUNMING INSTITUTE OF ZOOLOGY   (China)

Author keywords

Chelation; Flavonoid; HIV 1 integrase inhibitors; LEDGF p75; Strand transfer

Indexed keywords

2 (2,2 DIPHENYLBENZO[D][1,3]DIOXOL 5 YL) 3,5,7 TRIHYDROXY 4H CHROMEN 4 ONE; 2 (3,4 DIHYDROXYPHENYL) 3,5 DIHYDROXY 7 MORPHOLINO 4H CHROMEN 4 ONE; 2 (3,4 DIHYDROXYPHENYL) 5 HYDROXY 7 MORPHOLINO 4H CHROMEN 4 ONE; 2 (3,4 DIHYDROXYPHENYL) 7 [(4 FLUOROBENZYL)OXY] 3,5 DIHYDROXY 4H CHROMEN 4 ONE; 2 (3,4 DIHYDROXYPHENYL) 7 [(4 FLUOROBENZYL)OXY] 5 HYDROXY 4H CHROMEN 4 ONE; 5 HYDROXY 2 (4 HYDROXYPHENYL) 7 MORPHOLINO 4H CHROMEN 4 ONE; 5 HYDROXY 3 (4 HYDROXYPHENYL) 7 MORPHOLINO 4H CHROMEN 4 ONE; 5 HYDROXY 7 MORPHOLINO 2 PHENYL 4H CHROMEN 4 ONE; 7 (BUTOXY) 5 HYDROXY 2 (4 HYDROXYPHENYL) 4H CHROMEN 4 ONE; 7 (BUTOXY) 5 HYDROXY 2 PHENYL 4H CHROMEN 4 ONE; 7 (BUTOXY) 5 HYDROXY 3 (4 HYDROXYPHENYL) 4H CHROMEN 4 ONE; 7 [(4 FLUOROBENZYL)OXY] 5 HYDROXY 2 (4 HYDROXYPHENYL) 4H CHROMEN 4 ONE; 7 [(4 FLUOROBENZYL)OXY] 5 HYDROXY 2 PHENYLCHROMAN 4 ONE; 7 [(4 FLUOROBENZYL)OXY] 5 HYDROXY 3 (4 HYDROXYPHENYL) 4H CHROMEN 4 ONE; 7 [(4 FLUOROBENZYL)OXY] 5,6 DIHYDROXY 2 PHENYL 4H CHROMEN 4 ONE; APIGENIN; BAICALEIN; CHRYSIN; FLAVONOID; GENISTEIN; INTEGRASE INHIBITOR; LENS EPITHELIUM DERIVED GROWTH FACTOR; LUTEOLIN; NARINGENIN; PROTEIN P75; QUERCETIN; UNCLASSIFIED DRUG; 5-HYDROXY-3-(4-HYDROXYPHENYL)-7-MORPHOLINO-4H-CHROMEN-4-ONE; ANTIVIRUS AGENT; CHROMONE DERIVATIVE; INTEGRASE; MORPHOLINE DERIVATIVE; P31 INTEGRASE PROTEIN, HUMAN IMMUNODEFICIENCY VIRUS 1; PROTEIN V FOS; PSIP1 PROTEIN, HUMAN; SIGNAL TRANSDUCING ADAPTOR PROTEIN; TRANSCRIPTION FACTOR;

ANTIVIRAL ACTIVITY; ARTICLE; DRUG DESIGN; DRUG EFFICACY; DRUG PROTEIN BINDING; DRUG STRUCTURE; DRUG TARGETING; ENZYME ACTIVE SITE; ENZYME INHIBITION ASSAY; HUMAN IMMUNODEFICIENCY VIRUS 1 INFECTION; HYDROPHOBICITY; IC 50; PHYSICAL CHEMISTRY; PROCESS DEVELOPMENT; PROTEIN DOMAIN; CHEMICAL STRUCTURE; CHEMISTRY; DRUG DEVELOPMENT; DRUG EFFECTS; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; METABOLISM; STRUCTURE ACTIVITY RELATION; SYNTHESIS;

HUMAN IMMUNODEFICIENCY VIRUS 1;

ADAPTOR PROTEINS, SIGNAL TRANSDUCING; ANTIVIRAL AGENTS; CATALYTIC DOMAIN; CHROMONES; DRUG DESIGN; DRUG DISCOVERY; FLAVONOIDS; HIV INTEGRASE; HIV INTEGRASE INHIBITORS; HIV-1; HUMANS; MOLECULAR STRUCTURE; MORPHOLINES; ONCOGENE PROTEINS V-FOS; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSCRIPTION FACTORS;

EID: 84901233744     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2014.04.016     Document Type: Article

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