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Page 1
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: gu hh. J Med Chem. 2004 Aug 26;47(18):4517-29. doi: 10.1021/jm030217e. J Med Chem. 2004. PMID: 15317463
Novel diamide-based inhibitors of IMPDH.
Gu HH, Iwanowicz EJ, Guo J, Watterson SH, Shen Z, Pitts WJ, Dhar TG, Fleener CA, Rouleau K, Sherbina NZ, Witmer M, Tredup J, Hollenbaugh D. Gu HH, et al. Bioorg Med Chem Lett. 2002 May 6;12(9):1323-6. doi: 10.1016/s0960-894x(02)00132-4. Bioorg Med Chem Lett. 2002. PMID: 11965381
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: gu hh. 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
Rapid synthesis of triazine inhibitors of inosine monophosphate dehydrogenase.
Pitts WJ, Guo J, Dhar TG, Shen Z, Gu HH, Watterson SH, Bednarz MS, Chen BC, Barrish JC, Bassolino D, Cheney D, Fleener CA, Rouleau KA, Hollenbaugh DL, Iwanowicz EJ. Pitts WJ, et al. Among authors: gu hh. Bioorg Med Chem Lett. 2002 Aug 19;12(16):2137-40. doi: 10.1016/s0960-894x(02)00351-7. Bioorg Med Chem Lett. 2002. PMID: 12127522
Novel amide-based inhibitors of inosine 5'-monophosphate dehydrogenase.
Watterson SH, Liu C, Dhar TG, Gu HH, Pitts WJ, Barrish JC, Fleener CA, Rouleau K, Sherbina NZ, Hollenbaugh DL, Iwanowicz EJ. Watterson SH, et al. Among authors: gu hh. Bioorg Med Chem Lett. 2002 Oct 21;12(20):2879-82. doi: 10.1016/s0960-894x(02)00601-7. Bioorg Med Chem Lett. 2002. PMID: 12270168
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: gu hh. 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: gu hh. 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
Acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase: discovery and SAR leading to the identification of N-(2-(6-(4-ethylpiperazin-1-yl)pyridin-3-yl)propan-2-yl)-2- fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide (BMS-566419).
Watterson SH, Chen P, Zhao Y, Gu HH, Dhar TG, Xiao Z, Ballentine SK, Shen Z, Fleener CA, Rouleau KA, Obermeier M, Yang Z, McIntyre KW, Shuster DJ, Witmer M, Dambach D, Chao S, Mathur A, Chen BC, Barrish JC, Robl JA, Townsend R, Iwanowicz EJ. Watterson SH, et al. Among authors: gu hh. J Med Chem. 2007 Jul 26;50(15):3730-42. doi: 10.1021/jm070299x. Epub 2007 Jun 22. J Med Chem. 2007. PMID: 17585753
114 results