Lead identification of benzimidazolone and azabenzimidazolone arylsulfonamides as CC-chemokine receptor 4 (CCR4) antagonists

A knowledge-based library of 2,3-dichlorophenylsulfonyl derivatives of commercially available aryl amines was synthesised and screened as human CCR4 antagonists, in order to identify a suitable hit for the start of a lead-optimisation programme. Hits were required to be more potent than an existing...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2014-08, Vol.22 (15), p.4298-4311
Hauptverfasser:	Miah, Afjal H., Abas, Hossay, Begg, Malcolm, Marsh, Benjamin J., O’Flynn, Daniel E., Ford, Alison J., Percy, Jonathan M., Procopiou, Panayiotis A., Richards, Steve A., Rumley, Sally-Anne
Format:	Artikel
Sprache:	eng
Schlagworte:	Aza Compounds - chemistry Azabenzimidazolone Benzimidazoles - chemistry Benzimidazolone CCR4 antagonist Humans Indazoles - chemistry Protein Binding Receptors, CCR4 - antagonists & inhibitors Receptors, CCR4 - metabolism Serum Albumin - chemistry Serum Albumin - metabolism Structure-Activity Relationship Sulfonamides - chemical synthesis Sulfonamides - chemistry Sulfonamides - metabolism
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Zusammenfassung:	A knowledge-based library of 2,3-dichlorophenylsulfonyl derivatives of commercially available aryl amines was synthesised and screened as human CCR4 antagonists, in order to identify a suitable hit for the start of a lead-optimisation programme. Hits were required to be more potent than an existing indazole series, have better physicochemical properties (clogP
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2014.05.021