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Aza-stilbenes as potent and selective c-RAF inhibitors |
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| Authors: | McDonald Octerloney Lackey Karen Davis-Ward Ronda Wood Edgar Samano Vicente Maloney Patrick Deanda Felix Hunter Robert |
| Affiliation: | GlaxoSmithKline, Research Triangle Park, NC 27709, USA. |
| Abstract: | The synthesis of several novel aza-stilbene derivatives was carried out. The compounds were tested for their c-RAF enzyme inhibition. Compound 27 possesses significant potency against c-RAF and demonstrates selectivity over other protein kinases. A hypothesis for the binding mode, activity, and selectivity is proposed. |
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