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A new class of acyclic 2-alkyl-1,2-diaryl (E)-olefins as selective cyclooxygenase-2 (COX-2) inhibitors.

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 (IC(50)=0.77 microM) and selective (Selectivity Index>130) COX-2 inhibitor.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Uddin MJ,Rao PN,Rahim MA,McDonald R,Knaus EE

doi

10.1016/j.bmcl.2004.07.027

subject

Has Abstract

pub_date

2004-10-04 00:00:00

pages

4911-4

issue

19

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(04)00919-9

journal_volume

14

pub_type

杂志文章

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