Synthesis and Structure–Activity Relationships of Indazole Arylsulfonamides as Allosteric CC-Chemokine Receptor 4 (CCR4) Antagonists

…, DA Hall, AP Hancock, AP Hill, H Hobbs…

Index: Procopiou, Panayiotis A.; Barrett, John W.; Barton, Nicholas P.; Begg, Malcolm; Clapham, David; Copley, Royston C. B.; Ford, Alison J.; Graves, Rebecca H.; Hall, David A.; Hancock, Ashley P.; Hill, Alan P.; Hobbs, Heather; Hodgson, Simon T.; Jumeaux, Coline; Lacroix, Yannick M. L.; Miah, Afjal H.; Morriss, Karen M. L.; Needham, Deborah; Sheriff, Emma B.; Slack, Robert J.; Smith, Claire E.; Sollis, Steven L.; Staton, Hugo Journal of Medicinal Chemistry, 2013 , vol. 56, # 5 p. 1946 - 1960

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Citation Number: 12

Abstract

A series of indazole arylsulfonamides were synthesized and examined as human CCR4 antagonists. Methoxy-or hydroxyl-containing groups were the more potent indazole C4 substituents. Only small groups were tolerated at C5, C6, or C7, with the C6 analogues being preferred. The most potent N 3-substituent was 5-chlorothiophene-2-sulfonamide. N 1 meta-substituted benzyl groups possessing an α-amino-3-[(methylamino) acyl]–group ...