Synthesis and biological evaluation of 2-phenylquinolones targeted at Tat/TAR recognition

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 3, 2009, Pages 714-717

  Manfroni, Giuseppe ^a   Gatto, Barbara ^b   Tabarrini, Oriana ^a   Sabatini, Stefano ^a   Cecchetti, Violetta ^a   Giaretta, Giulia ^b   Parolin, Cristina ^b   Del Vecchio, Claudia ^b   Calistri, Arianna ^b   Palumbo, Manlio ^b   Fravolini, Arnaldo ^a  

^a UNIVERSITY OF PERUGIA   (Italy)

^b UNIVERSITY OF PADOVA   (Italy)

Author keywords

2 Phenylquinolones; Anti HIV agents; FQA; Tat TAR complex inhibitors

Indexed keywords

2 PHENYLQUINOLONE DERIVATIVE; BENZENE DERIVATIVE; QUINOLONE DERIVATIVE; TRANSACTIVATOR PROTEIN; UNCLASSIFIED DRUG;

ANTIVIRAL ACTIVITY; ARTICLE; BINDING COMPETITION; CONTROLLED STUDY; DRUG CYTOTOXICITY; DRUG DESIGN; DRUG SCREENING; DRUG SYNTHESIS; DRUG TARGETING; FLUORESCENCE ANALYSIS; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS 1; MOLECULAR RECOGNITION; NONHUMAN; PROTEIN RNA BINDING; STRUCTURE ACTIVITY RELATION;

ANTI-HIV AGENTS; CHEMISTRY, PHARMACEUTICAL; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; HUMANS; JURKAT CELLS; KINETICS; MODELS, CHEMICAL; PEPTIDE FRAGMENTS; QUINOLONES; RNA, VIRAL; SPECTROMETRY, FLUORESCENCE; TAT GENE PRODUCTS, HUMAN IMMUNODEFICIENCY VIRUS; TRANSCRIPTION, GENETIC;

EID: 58549111785     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.12.034     Document Type: Article

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25. i. A preliminary determination of the spectral parameters of all quinolones allowed us to exclude optical interferences with fluorescein-peptide signal at the conditions of the assay.
26. 3) in a microcentrifuge tube. The cell pellet was lysed overnight with 1 mL of 0.1 M glycine-HCl buffer (pH 3.0) and then the samples were centrifuged for 5 min at 5600g. The amount of compound in the lysis supernatant was determined by fluorescence directly in glycine buffer at pH 3, conditions at which it is possible to experimentally determine a titration curve for each quinolone. Controls without quinolones were always used to determine the background fluorescence.