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35248820467
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note
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The EGFR was purchased from Upstate (Active EGFR, Cat. No. 14-531) and used directly without further purification. Kinase assay experiments were performed according to the procedure as described in the booklet.
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0030039555
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Bridges A.J., Zhou H., Cody D.R., Rewcastle G.W., McMichael A., Showalter H.D.H., Fry D.W., Kraker A.J., and Denny W.A. J. Med. Chem. 39 (1996) 267
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19
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0035939330
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Barker, A.J.1
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20
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33746196584
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Petrov K.G., Zhang Y.-M., Carter M., Cockerill G.S., Dickerson S., Gauthier C.A., Guo Y., Mook Jr. R.A., Rusnak D.W., Walker A.L., Wood E.R., and Lackey K.E. Bioorg. Med. Chem. Lett. 16 (2006) 4686
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33644974478
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Some cases of C-3′ ethynyl-substituted 4-anilinoquinazoline derivatives, see:
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Some cases of C-3′ ethynyl-substituted 4-anilinoquinazoline derivatives, see:. Waterson A.G., Stevens K.L., Reno M.J., Zhang Y.-M., Boros E.E., Bouvier F., Rastagar A., Uehling D.E., Dickerson S.H., Reep B., McDonald O.B., Wood E.R., Rusnak D.W., Alligood K.J., and Rudolph S.K. Bioorg. Med. Chem. Lett. 14 (2006) 2419
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Waterson, A.G.1
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Boros, E.E.5
Bouvier, F.6
Rastagar, A.7
Uehling, D.E.8
Dickerson, S.H.9
Reep, B.10
McDonald, O.B.11
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Alligood, K.J.14
Rudolph, S.K.15
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35248869097
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note
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+.
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23
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35248839887
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33P] MgAc/ATP cocktail containing magnesium acetate (50 mM) and ATP (500 μM). The reaction mixture of a total volume of 25 μl was incubated at 30 °C for 30 min. Five microliters of phosphoric acid (3%) was added to stop the reaction. An aliquot of 20 μl from reaction was transferred onto the center of a 2 cm × 2 cm P81 paper and allow the radiolabeled substrate to bind to the filter paper for 30 s. Wash the assay squares five times for 5 min with water. Transfer the assay squares to vial and add 5 ml scintillation cocktail. Read in scintillation counter by Beckman LS-6500 counter.
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35248836350
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Docking modeling was applied to assist SAR study. Briefly, the 3D structure of EGFR (pdb coded 2ito) was obtained from RCSB Protein Data Bank (http://www.rcsb.org/pdb/home/home.do). The structures of three compounds (Tarceva, 5e, and 6b) were generated and the energies were optimized on Meastro by using Ligpre (Schrödinger, USA). Molecular docking was conducted by using Glide with XP mode (detailed in user manual of Schrödinger), which allows flexible conformational search of the compounds against the target. For each inhibitor, five best docking modes were generated and its final interacting complex with EGFR was selected based on computed docking score of Glide.
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35248835888
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Glide docking scores of Iressa (-9.44), Tarceva (-10.83) as well as some active compounds such as 5e (-10.87), 6b (-9.88), and 6d (-3.42) showed that compound 5e is slightly favored over Iressa and Tarceva in EGFR kinase SAR.
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