2. Academic Validation
  3. Design, synthesis, and evaluation of naphthalene-sulfonamide antagonists of human CCR8

Design, synthesis, and evaluation of naphthalene-sulfonamide antagonists of human CCR8

  • J Med Chem. 2007 Feb 8;50(3):566-84. doi: 10.1021/jm061118e.
Tracy J Jenkins 1,  Bing Guan,  Mingshi Dai,  Gang Li,  Thomas E Lightburn,  Shan Huang,  B Scott Freeze,  Douglas F Burdi,  Swanee Jacutin-Porte,  Robert Bennett,  Weirong Chen,  Charles Minor,  Shomir Ghosh,  Christopher Blackburn,  Kenneth M Gigstad,  Matthew Jones,  Roland Kolbeck,  Wei Yin,  Sean Smith,  Daniel Cardillo,  Timothy D Ocain,  Geraldine C Harriman
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Department of Pharmacology, and Drug Safety and Disposition, Millennium Pharmaceuticals, 40 Landsdowne Street, Cambridge, Massachusetts 02139, USA. [email protected]
PMID: 17266208 DOI: 10.1021/jm061118e
Abstract

The design, synthesis, and structure-activity relationship development of naphthalene-derived human CCR8 antagonists is described. In vitro binding assay results of these investigations are reported, critical interactions of the antagonists with CCR8 are defined, and preliminary physicochemical and pharmacokinetic data for the naphthalene scaffold are presented.

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