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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Synthesis and SAR of pyrrolotriazine-4-one based Eg5 inhibitors.

Synthesis and SAR of substituted pyrrolotriazine-4-one analogues as Eg5 inhibitors are described. Many of these analogues displayed potent inhibitory activities in the Eg5 ATPase and A2780 cell proliferation assays. In addition, pyrrolotriazine-4-one analogue 26 demonstrated in vivo efficacy in an iv P388 murine leukemia model. Both NMR and X-ray crystallographic studies revealed that these analogues bind to an allosteric site on the Eg5 protein.[1]

References

  1. Synthesis and SAR of pyrrolotriazine-4-one based Eg5 inhibitors. Kim, K.S., Lu, S., Cornelius, L.A., Lombardo, L.J., Borzilleri, R.M., Schroeder, G.M., Sheng, C., Rovnyak, G., Crews, D., Schmidt, R.J., Williams, D.K., Bhide, R.S., Traeger, S.C., McDonnell, P.A., Mueller, L., Sheriff, S., Newitt, J.A., Pudzianowski, A.T., Yang, Z., Wild, R., Lee, F.Y., Batorsky, R., Ryder, J.S., Ortega-Nanos, M., Shen, H., Gottardis, M., Roussell, D.L. Bioorg. Med. Chem. Lett. (2006) [Pubmed]
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