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

Journal of Medicinal Chemistry

Volumn 50, Issue 3, 2007, Pages 566-584

  Jenkins, Tracy J ^a   Guan, Bing ^a   Dai, Mingshi ^a   Li, Gang ^a   Lightburn, Thomas E ^a   Huang, Shan ^a   Freeze, B Scott ^a   Burdi, Douglas F ^a   Jacutin Porte, Swanee ^a   Bennett, Robert ^a   Chen, Weirong ^a   Minor, Charles ^a   Ghosh, Shomir ^a   Blackburn, Christopher ^a   Gigstad, Kenneth M ^a   Jones, Matthew ^a   Kolbeck, Roland ^a   Yin, Wei ^a   Smith, Sean ^a   Cardillo, Daniel ^a   Ocain, Timothy D ^a   Harriman, Geraldine C ^a   more..

^a MILLENNIUM PHARMACEUTICALS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CHEMOKINE RECEPTOR ANTAGONIST; CHEMOKINE RECEPTOR CCR8; CHEMOKINE RECEPTOR CCR8 ANTAGONIST; N [4 (4 METHOXYPHENYLSULFAMOYL)NAPHTHALEN 1 YL] BENZAMIDE; NAPHTHALENE DERIVATIVE; SULFONAMIDE; UNCLASSIFIED DRUG;

ARTICLE; DRUG DESIGN; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; HYDROGEN BOND; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; BIOLOGICAL TRANSPORT; CALCIUM; CELL LINE; CRICETINAE; CRICETULUS; DRUG DESIGN; HUMANS; NAPHTHALENES; RATS; RECEPTORS, CHEMOKINE; SOLUBILITY; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES;

EID: 33846934641     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm061118e     Document Type: Article

References (22)

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17. 50) values. For clarity, SAR tables are organized using data from one or the other of these assays but not both.
18. Naphthalene core replacement results will be disclosed in a subsequent manuscript.
19. A table containing selected data from the Novascreen panel is presented in the Supporting Information section. Note that, although only select entries are reproduced here, compound 15 displayed <20% inhibition at 10 μM across all 40 receptors evaluated.
20. HEK-293 cells that were stably transfected with hERG cDNA were obtained according to Zhou, Z.; Gong, Q.; Ye, B.; Fan, Z.; Makielski, J. C.; Robertson, G. A. Biophys. J. 1998, 74, 230.
21. 2, and centrifuged at 4°C. The hERG binding assay was conducted as described in the following references: (a) Finlayson, K.; Sharkey, J. In Optimization in Drug Discovery; Yan, Z., Caldwell, G. W., Eds. Humana Press: Totowa, NJ, 2004; pp 353-368.
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