35748-36-8Relevant academic research and scientific papers
Design, synthesis and anti-tumor evaluation of 1,2,4-triazol-3-one derivatives and pyridazinone derivatives as novel CXCR2 antagonists
Chu, Bizhu,Jiang, Yuyang,Li, Qinyuan,Liu, Zijian,Luo, Jingyi,Shi, Zhichao,Xin, Qilei,Ye, Lizhen,Zhan, Feng,Zhang, Xun,Zhu, Qingyun
, (2021/09/20)
Chemokine receptor 2 (CXCR2) is the receptor of glutamic acid–leucine–arginine sequence-contained chemokines CXCs (ELR+ CXCs). In recent years, CXCR2-target treatment strategy has come a long way in cancer therapy. CXCR2 antagonists could block
Bicyclo[2.2.1]heptane containing: N, N ′-diarylsquaramide CXCR2 selective antagonists as anti-cancer metastasis agents
Che, Jin-Xin,Wang, Zhi-Long,Dong, Xiao-Wu,Hu, You-Hong,Xie, Xin,Hu, Yong-Zhou
, p. 11061 - 11069 (2018/03/26)
CXCR1 and CXCR2 are CXC chemokine receptors (CXCRs), corresponding to cytokines of the CXC chemokine family. CXCR2 was found to be 77% homologous to CXCR1. Antagonism of the chemokine receptor CXCR2 has been proposed as a new strategy for the treatment of
Early Development Scale-Up of a Novel CXCR Antagonist: Focus on Racemic and Stereoselective Routes of a Key Intermediate
Tabet, Samuel,Rodeville, Nicolas,Mathieu, Arnaud,Raffin, Catherine,Millois-Barbuis, Corinne,Musicki, Branislav,Muller, Franck,Gerfaud, Thibaud,Boiteau, Jean-Guy,Cardinaud, Isabelle
, p. 2032 - 2044 (2017/12/26)
Efforts toward a convenient and scalable process for the synthesis of a novel CXCR antagonist 1 are described, with a specific focus on a chiral key intermediate. Two generations of a racemic route have been developed for short-term deliveries, and a ster
An organotrifluoroborate-based convergent total synthesis of the potent cancer cell growth inhibitory depsipeptides kitastatin and respirantin
Beveridge, Ramsay E.,Batey, Robert A.
supporting information, p. 2322 - 2325 (2014/05/20)
The total syntheses of the highly cytotoxic neo-antimycin macrocyclic depsipeptide natural products kitastatin and respirantin have been accomplished in a convergent manner using MNBA promoted esterifications and an efficient C- and N-terminus bis-deprote
BICYCLIC RING SYSTEM SUBSTITUTED AMIDE FUNCTIONALISED PHENOLS AS MEDICAMENTS
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Page/Page column 34, (2012/06/30)
This invention relates to bicyclic ring system substituted amide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.
BICYCLIC RING SYSTEM SUBSTITUTED AMIDE FUNCTIONALISED PHENOLS AS MEDICAMENTS
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Page/Page column 19, (2013/02/28)
This invention relates to bicyclic ring system substituted amide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds
Synthesis of substituted benzoxazolinones by the curtius rearrangement: Crystal structures of Intermediates and by-products
Laus, Gerhard,Kahlenberg, Volker,Wurst, Klaus,Nerdinger, Sven,Schottenberger, Herwig
experimental part, p. 479 - 486 (2011/07/07)
3-Substituted salicyloyl chlorides were converted to salicyloyl azides (R = Br, NO2) which underwent thermal rearrangement and intramolecular cyclization to benzoxazolinones. The crystal structures of 7-substituted benz[d]oxazolin-2-ones (R = B
3, 4-DI-SUBSTITUTED CYCLOBUTENE- 1, 2 -DIONES AS CXCR2 RECEPTOR ANTAGONISTS
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Page/Page column 41-42, (2010/06/20)
The present invention relates to compounds of formula (I) wherein R1, R2, Ar, p, R4 and R5 are as defined herein, which are useful for creating diseases which respond to CXCR2 receptor mediators. Pharmaceutical
3,4-DI-SUBSTITUTED CYCLOBUTENE-1,2-DIONES AS CXC-CHEMOKINE RECEPTOR LIGANDS
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Page/Page column 69-70, (2008/06/13)
Disclosed are novel cyclobutenedione Compounds comprising a cycloclobutenedione ring, a substituted phenyl ring, and a -CH(C2H5)-furan moiety. The phenyl ring and the -CH(C2H5)-furan moiety are each bound to the
C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists
Chao, Jianhua,Taveras, Arthur G.,Chao, Jianping,Aki, Cynthia,Dwyer, Michael,Yu, Younong,Purakkattle, Biju,Rindgen, Diane,Jakway, James,Hipkin, William,Fosetta, James,Fan, Xuedong,Lundell, Daniel,Fine, Jay,Minnicozzi, Michael,Phillips, Jonathan,Merritt, J. Robert
, p. 3778 - 3783 (2008/02/10)
A novel series of cyclobutenedione centered C(4)-alkyl substituted furanyl analogs was developed as potent CXCR2 and CXCR1 antagonists. Compound 16 exhibits potent inhibitory activities against IL-8 binding to the receptors (CXCR2 Ki = 1 nM, IC50 = 1.3 nM; CXCR1 Ki = 3 nM, IC50 = 7.3 nM), and demonstrates potent inhibition against both Gro-α and IL-8 induced hPMN migration (chemotaxis: CXCR2 IC50 = 0.5 nM, CXCR1 IC50 = 37 nM). In addition, 16 has shown good oral pharmacokinetic profiles in rat, mouse, monkey, and dog.
