| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1366564 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
The identification, optimization, and structure–activity relationship (SAR) of small-molecule CCR4 antagonists is described. An initial screening hit with micromolar potency was identified that was optimized to sub-micromolar binding potency by enantiomer resolution, halogenation of the naphthalene ring, and extension of the alkyl chain linker between the central piperidine ring and the terminal aryl group. An antagonist was identified that showed good cross-reactivity against the mouse receptor and inhibited CCR4-based cell recruitment in dose-dependent fashion.
Graphical abstractThe identification, optimization, and structure–activity relationship (SAR) of small-molecule CCR4 antagonists is described. An antagonist 33 was identified that showed good cross-reactivity against the mouse receptor and inhibited CCR4-based cell recruitment in dose-dependent fashion.Figure optionsDownload full-size imageDownload as PowerPoint slide
