Literature DB >> 17181143

Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.

Michael P Dwyer1, Younong Yu, Jianping Chao, Cynthia Aki, Jianhua Chao, Purakkattle Biju, Viyyoor Girijavallabhan, Diane Rindgen, Richard Bond, Rosemary Mayer-Ezel, James Jakway, R William Hipkin, James Fossetta, Waldemar Gonsiorek, Hong Bian, Xuedong Fan, Carol Terminelli, Jay Fine, Daniel Lundell, J Robert Merritt, Laura L Rokosz, Bernd Kaiser, Ge Li, Wei Wang, Tara Stauffer, Lynne Ozgur, John Baldwin, Arthur G Taveras.   

Abstract

Structure-activity studies on lead cyclobutenedione 3 led to the discovery of 4 (SCH 527123), a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist with excellent cell-based activity. Compound 4 displayed good oral bioavailability in rat and may be a potential therapeutic agent for the treatment of various inflammatory diseases.

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Year:  2006        PMID： 17181143     DOI： 10.1021/jm0609622

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  30 in total

Review 1.  The CXCR1/2 Pathway: Involvement in Diabetes Pathophysiology and Potential Target for T1D Interventions.

Authors:  Antonio Citro; Elisa Cantarelli; Lorenzo Piemonti
Journal:  Curr Diab Rep       Date:  2015-10       Impact factor: 4.810

2.  SB-656933, a novel CXCR2 selective antagonist, inhibits ex vivo neutrophil activation and ozone-induced airway inflammation in humans.

Authors:  Aili L Lazaar; Lisa E Sweeney; Alexander J MacDonald; Neil E Alexis; Chao Chen; Ruth Tal-Singer
Journal:  Br J Clin Pharmacol       Date:  2011-08       Impact factor: 4.335

3.  Small molecule antagonists for CXCR2 and CXCR1 inhibit human colon cancer liver metastases.

Authors:  Michelle L Varney; Seema Singh; Aihua Li; Rosemary Mayer-Ezell; Richard Bond; Rakesh K Singh
Journal:  Cancer Lett       Date:  2010-10-29       Impact factor: 8.679

4.  Boronic acid-containing CXCR1/2 antagonists: Optimization of metabolic stability, in vivo evaluation, and a proposed receptor binding model.

Authors:  Dean Y Maeda; Angela M Peck; Aaron D Schuler; Mark T Quinn; Liliya N Kirpotina; Winston N Wicomb; Richard L Auten; Rambabu Gundla; John A Zebala
Journal:  Bioorg Med Chem Lett       Date:  2015-04-23       Impact factor: 2.823

5.  CXCR2 inhibition enhances sulindac-mediated suppression of colon cancer development.

Authors:  Yong Suk Lee; Dongwon Choi; Nam Yoon Kim; Sara Yang; Eunson Jung; Mingu Hong; Dongyun Yang; Heinz-Josef Lenz; Young-Kwon Hong
Journal:  Int J Cancer       Date:  2014-01-02       Impact factor: 7.396

Review 6.  Chemokine receptor antagonists: overcoming developmental hurdles.

Authors:  Richard Horuk
Journal:  Nat Rev Drug Discov       Date:  2008-12-12       Impact factor: 84.694

7.  Nicotinamide glycolates antagonize CXCR2 activity through an intracellular mechanism.

Authors:  Dean Y Maeda; Mark T Quinn; Igor A Schepetkin; Liliya N Kirpotina; John A Zebala
Journal:  J Pharmacol Exp Ther       Date:  2009-09-24       Impact factor: 4.030

8.  Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders.

Authors:  Heng Xu; Hongfu Lu; Zhongmiao Xu; Linbo Luan; Chengyong Li; Yan Xu; Kelly Dong; Jinqiang Zhang; Xiong Li; Yvonne Li; Gentao Liu; Sophie Gong; Yong-Gang Zhao; Ailian Liu; Yueting Zhang; Wei Zhang; Xin Cai; Jia-Ning Xiang; John D Elliott; Xichen Lin
Journal:  ACS Med Chem Lett       Date:  2016-02-08       Impact factor: 4.345

Review 9.  Emerging strategies for cancer immunoprevention.

Authors:  J C Roeser; S D Leach; F McAllister
Journal:  Oncogene       Date:  2015-09-14       Impact factor: 9.867

10.  Targeting lung inflammation: novel therapies for the treatment of COPD.

Authors:  Hongwei Yao; Willem I de Boer; Irfan Rahman
Journal:  Curr Respir Med Rev       Date:  2008
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