Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1365022 | Bioorganic & Medicinal Chemistry Letters | 2008 | 6 Pages |
Abstract
The design and synthesis of novel non-peptide CXCR4 antagonists is described. The peptide backbone of highly potent cyclic peptide-based CXCR4 antagonists was entirely replaced by an indole framework, which was expected to reproduce the disposition of the key pharmacophores consistent with those of potential bioactive conformations of the original peptides. A structure–activity relationship study on a series of modified indoles identified novel small-molecule antagonists having three pharmacophore functional groups through the appropriate linkers.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Satoshi Ueda, Manabu Kato, Shinsuke Inuki, Hiroaki Ohno, Barry Evans, Zi-xuan Wang, Stephen C. Peiper, Kazuki Izumi, Eiichi Kodama, Masao Matsuoka, Hideko Nagasawa, Shinya Oishi, Nobutaka Fujii,