Lead optimisation of the N1 substituent of a novel series of indazole arylsulfonamides as CCR4 antagonists and identification of a candidate for clinical investigation

Panayiotis A Procopiou; Alison J Ford; Rebecca H Graves; David A Hall; Simon T Hodgson; Yannick M L Lacroix; Deborah Needham; Robert J Slack

doi:10.1016/j.bmcl.2012.02.104

Lead optimisation of the N1 substituent of a novel series of indazole arylsulfonamides as CCR4 antagonists and identification of a candidate for clinical investigation

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2730-3. doi: 10.1016/j.bmcl.2012.02.104. Epub 2012 Mar 7.

Authors

Panayiotis A Procopiou¹, Alison J Ford, Rebecca H Graves, David A Hall, Simon T Hodgson, Yannick M L Lacroix, Deborah Needham, Robert J Slack

Affiliation

¹ Department of Medicinal Chemistry, Respiratory CEDD, GlaxoSmithKline Medicines Research Centre, Stevenage, Hertfordshire, United Kingdom. pan.a.procopiou@gsk.com

PMID: 22437117
DOI: 10.1016/j.bmcl.2012.02.104

Abstract

Synthesis and preliminary SAR of the N1 substituent of a novel series of indazole sulfonamide chemokine receptor 4 (CCR4) antagonist is reported. Compound 7r was identified for further development.

MeSH terms

Humans
Indazoles / chemical synthesis*
Indazoles / chemistry
Indazoles / pharmacology
Inhibitory Concentration 50
Molecular Structure
Protein Binding / drug effects
Receptors, Chemokine / antagonists & inhibitors*
Structure-Activity Relationship
Sulfonamides / chemical synthesis*
Sulfonamides / chemistry
Sulfonamides / pharmacology

Substances

Indazoles
Receptors, Chemokine
Sulfonamides