Literature DB >> 19647429

Novel CXCR3 antagonists with a piperazinyl-piperidine core.

Brian F McGuinness1, Carolyn DiIanni Carroll, Lisa Guise Zawacki, Guizhen Dong, Cangming Yang, Doug W Hobbs, Biji Jacob-Samuel, James W Hall, Chung-Her Jenh, Joseph A Kozlowski, Gopinadhan N Anilkumar, Stuart B Rosenblum.   

Abstract

High-throughput screening of an encoded combinatorial aryl piperazine library led to the identification of a novel series of potent piperazinyl-piperidine based CXCR3 antagonists. Analogs of the initial hit were synthesized via solid and solution phase methods to probe the influence of structure on the CXCR3 binding of these molecules. Various functional groups were found to contribute to the overall potency and essential molecular features were identified.

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Year:  2009        PMID: 19647429     DOI: 10.1016/j.bmcl.2009.07.020

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


  5 in total

Review 1.  Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.

Authors:  Roland E Dolle; Bertrand Le Bourdonnec; Karin Worm; Guillermo A Morales; Craig J Thomas; Wei Zhang
Journal:  J Comb Chem       Date:  2010-10-05

Review 2.  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

3.  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

4.  Metabolic profiling of ligands for the chemokine receptor CXCR3 by liquid chromatography-mass spectrometry coupled to bioaffinity assessment.

Authors:  Marija Mladic; Danny J Scholten; Maikel Wijtmans; David Falck; Rob Leurs; Wilfried M A Niessen; Martine J Smit; Jeroen Kool
Journal:  Anal Bioanal Chem       Date:  2015-07-12       Impact factor: 4.142

5.  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

  5 in total

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