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Page 1
Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56(Lck).
Chen P, Norris D, Iwanowicz EJ, Spergel SH, Lin J, Gu HH, Shen Z, Wityak J, Lin TA, Pang S, De Fex HF, Pitt S, Shen DR, Doweyko AM, Bassolino DA, Roberge JY, Poss MA, Chen BC, Schieven GL, Barrish JC. Chen P, et al. Among authors: norris d. Bioorg Med Chem Lett. 2002 May 20;12(10):1361-4. doi: 10.1016/s0960-894x(02)00191-9. Bioorg Med Chem Lett. 2002. PMID: 11992777
Novel inhibitors of IMPDH: a highly potent and selective quinolone-based series.
Watterson SH, Carlsen M, Dhar TG, Shen Z, Pitts WJ, Guo J, Gu HH, Norris D, Chorba J, Chen P, Cheney D, Witmer M, Fleener CA, Rouleau K, Townsend R, Hollenbaugh DL, Iwanowicz EJ. Watterson SH, et al. Among authors: norris d. Bioorg Med Chem Lett. 2003 Feb 10;13(3):543-6. doi: 10.1016/s0960-894x(02)00944-7. Bioorg Med Chem Lett. 2003. PMID: 12565968
Quinolone-based IMPDH inhibitors: introduction of basic residues on ring D and SAR of the corresponding mono, di and benzofused analogues.
Dhar TG, Watterson SH, Chen P, Shen Z, Gu HH, Norris D, Carlsen M, Haslow KD, Pitts WJ, Guo J, Chorba J, Fleener CA, Rouleau KA, Townsend R, Hollenbaugh D, Iwanowicz EJ. Dhar TG, et al. Among authors: norris d. Bioorg Med Chem Lett. 2003 Feb 10;13(3):547-51. doi: 10.1016/s0960-894x(02)00945-9. Bioorg Med Chem Lett. 2003. PMID: 12565969
Identification of novel and potent isoquinoline aminooxazole-based IMPDH inhibitors.
Chen P, Norris D, Haslow KD, Murali Dhar TG, Pitts WJ, Watterson SH, Cheney DL, Bassolino DA, Fleener CA, Rouleau KA, Hollenbaugh DL, Townsend RM, Barrish JC, Iwanowicz EJ. Chen P, et al. Among authors: norris d. Bioorg Med Chem Lett. 2003 Apr 7;13(7):1345-8. doi: 10.1016/s0960-894x(03)00107-0. Bioorg Med Chem Lett. 2003. PMID: 12657279
Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.
Chen P, Doweyko AM, Norris D, Gu HH, Spergel SH, Das J, Moquin RV, Lin J, Wityak J, Iwanowicz EJ, McIntyre KW, Shuster DJ, Behnia K, Chong S, de Fex H, Pang S, Pitt S, Shen DR, Thrall S, Stanley P, Kocy OR, Witmer MR, Kanner SB, Schieven GL, Barrish JC. Chen P, et al. Among authors: norris d. J Med Chem. 2004 Aug 26;47(18):4517-29. doi: 10.1021/jm030217e. J Med Chem. 2004. PMID: 15317463
Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.
Chen P, Norris D, Das J, Spergel SH, Wityak J, Leith L, Zhao R, Chen BC, Pitt S, Pang S, Shen DR, Zhang R, De Fex HF, Doweyko AM, McIntyre KW, Shuster DJ, Behnia K, Schieven GL, Barrish JC. Chen P, et al. Among authors: norris d. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6061-6. doi: 10.1016/j.bmcl.2004.09.093. Bioorg Med Chem Lett. 2004. PMID: 15546730
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.
Lombardo LJ, Lee FY, Chen P, Norris D, Barrish JC, Behnia K, Castaneda S, Cornelius LA, Das J, Doweyko AM, Fairchild C, Hunt JT, Inigo I, Johnston K, Kamath A, Kan D, Klei H, Marathe P, Pang S, Peterson R, Pitt S, Schieven GL, Schmidt RJ, Tokarski J, Wen ML, Wityak J, Borzilleri RM. Lombardo LJ, et al. Among authors: norris d. J Med Chem. 2004 Dec 30;47(27):6658-61. doi: 10.1021/jm049486a. J Med Chem. 2004. PMID: 15615512
2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor.
Das J, Chen P, Norris D, Padmanabha R, Lin J, Moquin RV, Shen Z, Cook LS, Doweyko AM, Pitt S, Pang S, Shen DR, Fang Q, de Fex HF, McIntyre KW, Shuster DJ, Gillooly KM, Behnia K, Schieven GL, Wityak J, Barrish JC. Das J, et al. Among authors: norris d. J Med Chem. 2006 Nov 16;49(23):6819-32. doi: 10.1021/jm060727j. J Med Chem. 2006. PMID: 17154512
1,441 results