Title of article
Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists
Author/Authors
An-Rong Li، نويسنده , , Michael G. Johnson، نويسنده , , Jiwen Liu، نويسنده , , Xiaoqi Chen، نويسنده , , Xiaohui Du، نويسنده , , Jeffrey T. Mihalic، نويسنده , , Jeffrey Deignan، نويسنده , , Darin J. Gustin، نويسنده , , Jason Duquette، نويسنده , , Zice Fu، نويسنده , , Liusheng Zhu، نويسنده , , Andrew P. Marcus، نويسنده , , Phillipe Bergeron، نويسنده , , Lawrence R. McGee، نويسنده , , Jay Danao، نويسنده , , Bryan Lemon، نويسنده , , Teresa Carabeo، نويسنده , , Timothy Sullivan، نويسنده , , Hong-Ji Ma and Rui Nie، نويسنده , , Liang Tang، نويسنده , , et al.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
6
From page
688
To page
693
Abstract
A series of six–six and six–five fused heterocyclic CXCR3 antagonists has been synthesized and their activities evaluated in an [125I]-IP-10 displacement assay and an ITAC mediated in vitro cell migration assay. The pharmacokinetic properties of several top compounds have also been studied. This effort led to the discovery of compounds with increased potency and improved pharmacokinetic properties that could serve as useful tools to study the role of the CXCR3 receptor in vivo.
Keywords
Chemokine , MIG , CXCR3 , ITAC , CXCL9 , CXCL10 , CXCL11 , IP10
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799041
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