2-Anilino-4-aryl-8H-purine derivatives as inhibitors of PDK1
2012
Blanchard, Stéphanie | Soh, Chang Kai | Lee, Chai Ping | Poulsen, Anders | Bonday, Zahid | Goh, Kay Lin | Goh, Kee Chuan | Goh, Miah Kiat | Pasha, Mohammed Khalid | Wang, Haishan | Williams, Meredith | Wood, Jeanette M. | Ethirajulu, Kantharaj | Dymock, Brian W.
A series of 2-anilino substituted 4-aryl-8H-purines were prepared as potent inhibitors of PDK1, a serine-threonine kinase thought to play a role in the PI3K/Akt signaling pathway, a key mediator of cancer cell growth, survival and tumorigenesis. The synthesis, SAR and ADME properties of this series of compounds are discussed culminating in the discovery of compound 6 which possessed sub-micromolar cell proliferation activity and 65% oral bioavailability in mice.
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