Bioorganic and Medicinal Chemistry Letters p. 2056 - 2060 (2013)
Update date:2022-09-26
Topics:
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.
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.
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