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Literature DB >> 24900538

Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.

Tao Wang¹, Michelle L Lamb¹, Michael H Block¹, Audrey Molina Davies¹, Yongxin Han², Ethan Hoffmann¹, Stephanos Ioannidis¹, John A Josey², Zhong-Ying Liu¹, Paul D Lyne¹, Terry MacIntyre¹, Peter J Mohr², Charles A Omer¹, Tove Sjögren³, Kenneth Thress¹, Bin Wang², Haiyun Wang¹, Dingwei Yu¹, Hai-Jun Zhang¹.

Abstract

Trk receptor tyrosine kinases have been implicated in cancer and pain. A crystal structure of TrkA with AZ-23 (1a) was obtained, and scaffold hopping resulted in two 5/6-bicyclic series comprising either imidazo[4,5-b]pyridines or purines. Further optimization of these two fusion series led to compounds with subnanomolar potencies against TrkA kinase in cellular assays. Antitumor effects in a TrkA-driven mouse allograft model were demonstrated with compounds 2d and 3a.

Entities: Chemical Disease Gene Species

Keywords: Trk; cancer; imidazo[4,5-b]pyridines; kinase inhibitors; purines

Year: 2012 PMID： 24900538 PMCID： PMC4025776 DOI： 10.1021/ml300074j

Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345

16 in total

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8. Identification and preclinical characterization of AZ-23, a novel, selective, and orally bioavailable inhibitor of the Trk kinase pathway.

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