68. In Vivo Efficacy of Natural Product-Inspired Irreversible Kinase Inhibitors
    S. Barluenga, R. Jogireddy, G. K. Koripelly, N. Winssinger
    Chem. Bio. Chem. 2010, 11, 1692-1699

Inspirational kinase inhibitors: The terminal inhibition achieved with irreversible inhibitors has frequently been harnessed by Nature. Resorcyclic acid lactones (RAL) bearing a cis-enone moiety have emerged as promising pharmacophores for kinase inhibition. Two prototypical edited RALs were evaluated on an orthotopic murine carcinoma. Despite their similar biochemical activity profile, remarkable differences were observed with respect to metastasis inhibition.

DOI : 10.1002/cbic.201000205 

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