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

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.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2012-04, Vol.22 (8), p.2730-2733
Main Authors: Procopiou, Panayiotis A., Ford, Alison J., Graves, Rebecca H., Hall, David A., Hodgson, Simon T., Lacroix, Yannick M.L., Needham, Deborah, Slack, Robert J.
Format: Article
Language:English
Subjects:
Antagonist
Antagonists
Biological and medical sciences
CCR4
chemistry
Chemokine receptor 4
Chemokine receptors
chemokines
Humans
Indazoles - chemical synthesis
Indazoles - chemistry
Indazoles - pharmacology
Inhibitory Concentration 50
Lead
MDC
Medical sciences
Miscellaneous
Molecular Structure
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Protein Binding - drug effects
Receptors, Chemokine - antagonists & inhibitors
Structure-Activity Relationship
Sulfonamides
Sulfonamides - chemical synthesis
Sulfonamides - chemistry
Sulfonamides - pharmacology
TARC
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Description
Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.02.104