| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371678 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
A set of phenyl-substituted Smac mimetics/IAP inhibitor analogues of lead compound 2a was synthesized, aiming to retain its strong cell-free potency while increasing its bioavailability. Seventeen compounds 2b–r were prepared and characterized in vitro, using cell-free and cellular assays. Among them, the p-CF3 substituted analogue 2m showed the best permeability through cell membranes, and was selected for further in vitro and in vivo studies due to its strong, sub-micromolar cellular potency.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Aldo Bianchi, Marcello Ugazzi, Luca Ferrante, Daniele Lecis, Cinzia Scavullo, Eloise Mastrangelo, Pierfausto Seneci,