1428226-75-8Relevant academic research and scientific papers
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.
