Design, synthesis and evaluation of potent thymidylate synthase X inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 12, 2008, Pages 3628-3631

  Esra Onen F ^a,b,c,d,e   Boum, Yap ^f   Jacquement, Claire ^a,b,c,d,e   Spanedda, Maria Vittoria ^a,b,c,d,e   Jaber, Nada ^a,b,c,d,e   Scherman, Daniel ^a,b,c,d,e   Myllykallio, Hannu ^f   Herscovici, Jean ^a,b,c,d,e  

^a PSL RESEARCH UNIVERSITY   (France)

^b UNIVERSITÉ PARIS DESCARTES   (France)

^c CNRS   (France)

^d INSERM   (France)

^e UFR des Sciences Exactes et Naturelles   (France)

^f UNIVERSITÉ PARIS SACLAY   (France)

Author keywords

Antibacterial; Click chemistry; Thiazolidine; Thymidilate synthase; Triazole

Indexed keywords

THYMIDYLATE SYNTHASE INHIBITOR;

ARTICLE; CATALYSIS; CHEMICAL REACTION; DRUG DESIGN; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME INHIBITION;

DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; MOLECULAR CONFORMATION; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLIDINES; THYMIDYLATE SYNTHASE; TIME FACTORS;

EID: 44649153722     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.04.080     Document Type: Article

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15. 340 (due to oxidation of NADPH) that was measured with a reading interval of 30 s for duration of 15 min. All assays used a kinetic mode of a multilabel microplate reader [CHAMELEON II (Hidex, Finland)] with an injector. All screening reactions were performed in triplicates. The primary screen was performed with the small molecules dissolved in DMSO, including DMSO alone as low-activity control. The concentration of screened compounds was 20 μM unless otherwise indicated. Dose-response curves of the chosen compounds were determined using a wide range of compounds.
16. +. Purity by ELSD 99%.
17. +. Purity by ELSD 99%.