Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3

https://doi.org/10.1016/j.bmcl.2007.03.106Get rights and content

Abstract

A series of quinazolinone-derived inhibitors of the CXCR3 receptor have been synthesized and their affinity for the receptor evaluated. Compounds were evaluated in a 125I-IP10 displacement assay and in in vitro cell migration assays to IP10, ITAC, and MIG using human peripheral blood mononuclear cells.

References and notes (17)

  • D.D. Patel et al.

    Clin. Immunol.

    (2001)
  • J.C. Medina et al.

    Ann. Rep. Med. Chem.

    (2005)
    S. Storelli et al.

    Bioorg. Med. Chem. Lett.

    (2005)
    A.G. Cole et al.

    Bioorg. Med. Chem. Lett.

    (2006)
    D.R. Allen et al.

    Bioorg. Med. Chem. Lett.

    (2007)
  • (a)Schall, T. J.; Dairaghi, D. J.; McMaster, B. E. WO Patent 16114,...(b)Medina, J. C.; Johnson, M. G.; Li, A. -R.; Liu, J.; Huang, A.; Zhu, L.; Marcus, A. P. WO Patent 083143,...
  • S. Qin et al.

    J. Clin. Invest.

    (1998)
  • L. Trentin et al.

    J. Clin. Invest.

    (1999)
  • D.L. Hodge et al.

    J. Immunol.

    (2002)
  • H. Yagi et al.

    J. Invest. Dermatol.

    (2003)
There are more references available in the full text version of this article.

Cited by (0)

†

Alan Huang, Gilead Sciences, Inc., Foster City, CA 94404; Andrew Marcus, University of California-Berkeley, Berkeley, CA 94720; Feng Xu, XenoPort Inc., Santa Clara, CA 94404; Jeff Kumer, Sunesis Pharmaceuticals Inc., South San Francisco, CA 94080; Chris Lawrence, Xencor, Monrovia, CA, 91016.

View full text
Copyright © 2007 Elsevier Ltd. All rights reserved.