Title of article
A new class of acyclic 2-alkyl-1,2-diaryl (E)-olefins as selective cyclooxygenase-2 (COX-2) inhibitors
Author/Authors
Md. Jashim Uddin، نويسنده , , P.N. Praveen Rao، نويسنده , , Md. Abdur Rahim، نويسنده , , E. Robert McDonald، نويسنده , , Edward E. Knaus، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
4
From page
4911
To page
4914
Abstract
A new class of (E)-2-alkyl-2-(4-methanesulfonylphenyl)-1-phenylethenes were designed for evaluation as selective cyclooxygense-2 (COX-2) inhibitors. The target olefins were synthesized, via a Takeda olefination reaction, followed by oxidation of the respective thiomethyl olefinic intermediate. In vitro COX-1/COX-2 inhibition studies identified (E)-2-(4-methanesulfonylphenyl)-1-phenyloct-1-ene (8d) as a potent (IC50 = 0.77 μM) and selective (Selectivity Index > 130) COX-2 inhibitor.
Keywords
fax: +1-780-492-1217 , (E)-Olefins , Molecular modeling.* Corresponding author. Tel.: +1-780-492-5993 , COX-2 inhibitors , e-mail: eknaus@pharmacy.ualberta.ca
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794898
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