Rubber-elasticity and electrochemical activity of iron(ii) tris(bipyridine) crosslinked poly(dimethylsiloxane) networks.

2,2'-Bipyridine-terminated poly(dimethylsiloxane)s (bpyPDMS) with number average molecular weights, M, of 3300, 6100, 26 200, and 50 000 g mol were synthesized. When mixed with Fe(BF) at low concentrations, red solutions formed with UV-vis spectra that match those of iron(ii) tris(2,2'-bipyridine) (Fe(bpy)). Upon solvent evaporation, Fe(bpy) crosslinked PDMS networks (bpyPDMS/Fe(ii)) formed, and were studied using oscillating shear rheometry.

SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo.

Purpose: The Aurora family of serine/threonine kinases (Aurora-A, Aurora-B, and Aurora-C) plays a key role in cells orderly progression through mitosis. Elevated expression levels of Aurora kinases have been detected in a high percentage of melanoma, colon, breast, ovarian, gastric, and pancreatic tumors. We characterized the biological and pharmacological properties of SNS-314, an ATP-competitive, selective, and potent inhibitor of Aurora kinases.

2-Aminobenzimidazoles as potent Aurora kinase inhibitors.

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 as a bioisostere of the biaryl urea residue of SNS-314 (1c), which is a potent Aurora kinase inhibitor and entered clinical testing in patients with solid tumors. Compared to SNS-314, this series of compounds offers better aqueous solubility while retaining comparable in vitro potency in biochemical and cell-based assays; in particular, 6m has also demonstrated a comparable mouse iv PK profile to SNS-314.