A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity: design, synthesis, and biological activity |
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| Authors: | Hughes Terry V Xu Guozhang Wetter Steven K Connolly Peter J Emanuel Stuart L Karnachi Prabha Pollack Scott R Pandey Niranjan Adams Mary Moreno-Mazza Sandra Middleton Steven A Greenberger Lee M |
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| Affiliation: | aJohnson & Johnson Pharmaceutical Research and Development, L.L.C., PO Box 300, 1000 Route 202, Raritan, NJ 08869, USA |
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| Abstract: | A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine was synthesized and found to have potent dual EGFR/HER2 kinase inhibitory activity. The structure-based drug design of this molecule as well as the kinase and cellular inhibition of HER2 kinase dependent cell lines will be discussed. |
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| Keywords: | EGFR HER2 HER1 Kinase Pyrimidine Quinazoline mimic Intramolecular hydrogen bond Restricted rotation Oxadiazole |
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