1000341-55-8Relevant articles and documents
AMINOPYRIMIDINE COMPOUNDS AS INHIBITORS OF T790M CONTAINING EGFR MUTANTS
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Page/Page column 135, (2014/06/11)
This invention relates to novel compounds of formula (I) which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer. (Formula I)
N-substituted azaindoles as potent inhibitors of Cdc7 kinase
Bryan, Marian C.,Falsey, James R.,Frohn, Mike,Reichelt, Andreas,Yao, Guomin,Bartberger, Michael D.,Bailis, Julie M.,Zalameda, Leeanne,Miguel, Tisha San,Doherty, Elizabeth M.,Allen, John G.
, p. 2056 - 2060 (2013/05/09)
Cdc7 kinase is responsible for the initiation and regulation of DNA replication and has been proposed as a target for cancer therapy. We have identified a class of Cdc7 inhibitors based on a substituted indole core. Synthesis of focused indole and azaindole analogs yielded potent and selective 5-azaindole Cdc7 inhibitors with improved intrinsic metabolic stability (ie 36). In parallel, quantum mechanical conformational analysis helped to rationalize SAR observations, led to a proposal of the preferred binding conformation in the absence of co-crystallography data, and allowed the design of 7-azaindole 37 as a second lead in this series.