Literature DB >> 20483605

Discovery of a novel series of CXCR3 antagonists.

Stefano Crosignani1, Marc Missotten, Christophe Cleva, Ruggero Dondi, Yann Ratinaud, Yves Humbert, Ashis Baran Mandal, Agnès Bombrun, Christine Power, André Chollet, Amanda Proudfoot.   

Abstract

The discovery of a novel series of CXCR3 antagonists is described. Starting from an HTS positive, iterative optimization gave potent compounds (IC(50) 15 nM in a chemotaxis assay). The strategy employed to improve the metabolic stability of these derivatives is described. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20483605     DOI： 10.1016/j.bmcl.2010.04.113

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


  3 in total

Review 1.  Molecular mechanisms of liver metastasis.

Authors:  Kenji Kawada; Suguru Hasegawa; Teppei Murakami; Yoshiro Itatani; Hisahiro Hosogi; Masahiro Sonoshita; Takanori Kitamura; Teruaki Fujishita; Masayoshi Iwamoto; Takuya Matsumoto; Ryo Matsusue; Koya Hida; Gaku Akiyama; Kae Okoshi; Masahiro Yamada; Junichiro Kawamura; Makoto Mark Taketo; Yoshiharu Sakai
Journal:  Int J Clin Oncol       Date:  2011-08-17       Impact factor: 3.402

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.  Computational Study of C-X-C Chemokine Receptor (CXCR)3 Binding with Its Natural Agonists Chemokine (C-X-C Motif) Ligand (CXCL)9, 10 and 11 and with Synthetic Antagonists: Insights of Receptor Activation towards Drug Design for Vitiligo.

Authors:  Giovanny Aguilera-Durán; Antonio Romo-Mancillas
Journal:  Molecules       Date:  2020-09-25       Impact factor: 4.411
  3 in total

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