1373557-80-2Relevant academic research and scientific papers
2-Anilino-4-aryl-8H-purine derivatives as inhibitors of PDK1
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.
, p. 2880 - 2884 (2012/05/20)
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.
