Literature DB >> 21109432

Synthesis and SAR of novel CXCR4 antagonists that are potent inhibitors of T tropic (X4) HIV-1 replication.

Renato Skerlj1, Gary Bridger, Ernie McEachern, Curtis Harwig, Chris Smith, Trevor Wilson, Duane Veale, Helen Yee, Jason Crawford, Krystyna Skupinska, Rossana Wauthy, Wen Yang, Yongbao Zhu, David Bogucki, Maria Di Fluri, Jonathon Langille, Dana Huskens, Erik De Clercq, Dominique Schols.   

Abstract

An early lead from the AMD070 program was optimized and a structure-activity relationship was developed for a novel series of heterocyclic containing compounds. Potent CXCR4 antagonists were identified based on anti-HIV-1 activity and Ca(2+) flux inhibition that displayed good pharmacokinetics in rat and dog.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 21109432     DOI： 10.1016/j.bmcl.2010.11.023

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


  9 in total

Review 1.  Drug discovery research targeting the CXC chemokine receptor 4 (CXCR4).

Authors:  Won-Tak Choi; Srinivas Duggineni; Yan Xu; Ziwei Huang; Jing An
Journal:  J Med Chem       Date:  2011-12-02       Impact factor: 7.446

2.  Synthesis of Novel Tetrahydroisoquinoline CXCR4 Antagonists with Rigidified Side-Chains.

Authors:  Edgars Jecs; Eric J Miller; Robert J Wilson; Huy H Nguyen; Yesim A Tahirovic; Brook M Katzman; Valarie M Truax; Michelle B Kim; Katie M Kuo; Tao Wang; Chi S Sum; Mary E Cvijic; Gretchen M Schroeder; Lawrence J Wilson; Dennis C Liotta
Journal:  ACS Med Chem Lett       Date:  2017-12-20       Impact factor: 4.345

3.  Predicting target-ligand interactions with graph convolutional networks for interpretable pharmaceutical discovery.

Authors:  Paola Ruiz Puentes; Laura Rueda-Gensini; Natalia Valderrama; Isabela Hernández; Cristina González; Laura Daza; Carolina Muñoz-Camargo; Juan C Cruz; Pablo Arbeláez
Journal:  Sci Rep       Date:  2022-05-19       Impact factor: 4.996

4.  Determination of the binding mode for the cyclopentapeptide CXCR4 antagonist FC131 using a dual approach of ligand modifications and receptor mutagenesis.

Authors:  S Thiele; J Mungalpara; A Steen; M M Rosenkilde; J Våbenø
Journal:  Br J Pharmacol       Date:  2014-12       Impact factor: 8.739

Review 5.  AMD3100/CXCR4 Inhibitor.

Authors:  Erik De Clercq
Journal:  Front Immunol       Date:  2015-06-08       Impact factor: 7.561

6.  An Agonist of the CXCR4 Receptor Strongly Promotes Regeneration of Degenerated Motor Axon Terminals.

Authors:  Samuele Negro; Giulia Zanetti; Andrea Mattarei; Alice Valentini; Aram Megighian; Giulia Tombesi; Alessandro Zugno; Valentina Dianin; Marco Pirazzini; Silvia Fillo; Florigio Lista; Michela Rigoni; Cesare Montecucco
Journal:  Cells       Date:  2019-09-30       Impact factor: 6.600

Review 7.  Small molecule inhibitors of CXCR4.

Authors:  Bikash Debnath; Shili Xu; Fedora Grande; Antonio Garofalo; Nouri Neamati
Journal:  Theranostics       Date:  2013-01-15       Impact factor: 11.556

8.  Discovery and characterization of novel small-molecule CXCR4 receptor agonists and antagonists.

Authors:  Rama K Mishra; Andrew K Shum; Leonidas C Platanias; Richard J Miller; Gary E Schiltz
Journal:  Sci Rep       Date:  2016-07-26       Impact factor: 4.379

9.  Synthetic Activators of Cell Migration Designed by Constructive Machine Learning.

Authors:  Dominique Bruns; Daniel Merk; Karthiga Santhana Kumar; Martin Baumgartner; Gisbert Schneider
Journal:  ChemistryOpen       Date:  2019-10-23       Impact factor: 2.911
  9 in total

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