We have identified a small-molecule inhibitor of tumor necrosis factor α (TNF-α) that promotes
subunit disassembly of this trimeric cytokine family member. The compound inhibits TNF-α …

This communication describes the discovery of a novel series of Aurora kinase inhibitors. Key
SAR and critical binding elements are discussed. Some of the more advanced analogues …

This Letter describes the discovery and key structure–activity relationship (SAR) of a series
of 2-aminobenzimidazoles as potent Aurora kinase inhibitors. 2-Aminobenzimidazole serves …

(+)-1,4-Dihydro-7-(trans-3-methoxy-4-methylamino-1-pyrrolidinyl)-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic
acid (voreloxin; formerly SNS-595 or AG-7352) is currently under …

Recent reports by Galeazzi and co-workers demonstrated the susceptibility of Aβ(1-42) to
undergo dityrosine formation via peroxidase-catalyzed tyrosine cross-linking. We have formed …

Since peroxidase-catalyzed dityrosine formation is inefficient for peptides, we have
developed alternative conditions for intermolecular dityrosine formation using the Miyaura−Suzuki …

A series of 2-amino-pyrazolopyridines was designed and synthesized as Polo-like kinase (Plk)
inhibitors based on a low micromolar hit. The SAR was developed to provide compounds …

Indolocarbazole glycosides related to rebeccamycin represent a promising category of
antitumor agents targeting DNA and topoisomerase I. These drugs prefer to adopt a closed …

A versatile, one-pot synthesis of 2-arylimidazole-4-carboxylic acids from arylamidines and
methyl-2-chloroacetoacetate is described. The transformation is chemoselective, and reaction …

The MetJ repressor is the archetypal example of the β-ribbon-helix-helix DNA binding motif.
A model of the MetJ β-ribbon (residues 22–28) was prepared by forming a dityrosine …