Pyrimido[4,5‐d]pyrimidin‐4(1H)‐one Derivatives as Selective Inhibitors of EGFR Threonine790 to Methionine790 (T790M) Mutants

Catching the mutants: Pyrimido[4,5-d]pyrimidin-4(1H)-one derivatives (see example) were identified as specific inhibitors of EGFRT790M mutants. The compounds bound with T790M or L858R/T790M mutants with significantly lower Kd values than that with EGFRWT. They also selectively inhibited EGFR signal transduction and proliferation of NSCLC cells harboring EGFRL858R/T790M mutation, but were significantly less potent to cells with EGFRWT. As a service to our authors and readers, this journal provides supporting information supplied by the authors. Such materials are peer reviewed and may be re-organized for online delivery, but are not copy-edited or typeset. Technical support issues arising from supporting information (other than missing files) should be addressed to the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.