Literature DB >> 18242988

Discovery of small molecule benzimidazole antagonists of the chemokine receptor CXCR3.

Martin E Hayes1, Grier A Wallace, Pintipa Grongsaard, Agnieszka Bischoff, Dawn M George, Wenyan Miao, Michael J McPherson, Robert H Stoffel, David W Green, Gregory P Roth.   

Abstract

High-throughput screening identified a low molecular weight antagonist of CXCR3 displaying micromolar activity in a membrane filtration-binding assay. Systematic modification of the benzimidazole core and tethered acetophenone moiety established tractable SAR of analogs with improved physicochemical properties and sub-micromolar activity across both human and murine receptors.

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Year:  2008        PMID: 18242988     DOI: 10.1016/j.bmcl.2008.01.074

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

1.  CXCR3 promotes plaque formation and behavioral deficits in an Alzheimer's disease model.

Authors:  Marius Krauthausen; Markus P Kummer; Julian Zimmermann; Elisabet Reyes-Irisarri; Dick Terwel; Bruno Bulic; Michael T Heneka; Marcus Müller
Journal:  J Clin Invest       Date:  2014-12-15       Impact factor: 14.808

2.  A selective and potent CXCR3 antagonist SCH 546738 attenuates the development of autoimmune diseases and delays graft rejection.

Authors:  Chung-Her Jenh; Mary Ann Cox; Long Cui; Eva-Pia Reich; Lee Sullivan; Shu-Cheng Chen; David Kinsley; Shiguang Qian; Seong Heon Kim; Stuart Rosenblum; Joseph Kozlowski; Jay S Fine; Paul J Zavodny; Daniel Lundell
Journal:  BMC Immunol       Date:  2012-01-10       Impact factor: 3.615

3.  CXCR3 antagonist VUF10085 binds to an intrahelical site distinct from that of the broad spectrum antagonist TAK-779.

Authors:  Belinda Nedjai; Jonathan M Viney; Hubert Li; Caroline Hull; Caroline A Anderson; Tomoki Horie; Richard Horuk; Nagarajan Vaidehi; James E Pease
Journal:  Br J Pharmacol       Date:  2015-02-10       Impact factor: 8.739

4.  NF-κB signaling regulates cell-autonomous regulation of CXCL10 in breast cancer 4T1 cells.

Authors:  Won Jong Jin; Bongjun Kim; Darong Kim; Hea-Young Park Choo; Hong-Hee Kim; Hyunil Ha; Zang Hee Lee
Journal:  Exp Mol Med       Date:  2017-02-17       Impact factor: 8.718

5.  One-Pot Two-Step Synthesis of 2-Aryl benzimidazole N-oxides Using Microwave Heating as a Tool.

Authors:  Fabrizio Politano; Ana K Gran-Magano; Nicholas E Leadbeater
Journal:  Molecules       Date:  2019-10-09       Impact factor: 4.411

6.  Design and Synthesis of Benzimidazole-Chalcone Derivatives as Potential Anticancer Agents.

Authors:  Cheng-Ying Hsieh; Pi-Wen Ko; Yu-Jui Chang; Mohit Kapoor; Yu-Chuan Liang; Hui-Hsien Lin; Jia-Cherng Horng; Ming-Hua Hsu
Journal:  Molecules       Date:  2019-09-06       Impact factor: 4.411

  6 in total

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