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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: schieven gl. 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
Discovery of highly potent, selective, covalent inhibitors of JAK3.
Kempson J, Ovalle D, Guo J, Wrobleski ST, Lin S, Spergel SH, Duan JJ, Jiang B, Lu Z, Das J, Yang BV, Hynes J Jr, Wu H, Tokarski J, Sack JS, Khan J, Schieven G, Blatt Y, Chaudhry C, Salter-Cid LM, Fura A, Barrish JC, Carter PH, Pitts WJ. Kempson J, et al. Bioorg Med Chem Lett. 2017 Oct 15;27(20):4622-4625. doi: 10.1016/j.bmcl.2017.09.023. Epub 2017 Sep 11. Bioorg Med Chem Lett. 2017. PMID: 28927786
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: schieven gl. 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: schieven gl. 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
The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.
Leftheris K, Ahmed G, Chan R, Dyckman AJ, Hussain Z, Ho K, Hynes J Jr, Letourneau J, Li W, Lin S, Metzger A, Moriarty KJ, Riviello C, Shimshock Y, Wen J, Wityak J, Wrobleski ST, Wu H, Wu J, Desai M, Gillooly KM, Lin TH, Loo D, McIntyre KW, Pitt S, Shen DR, Shuster DJ, Zhang R, Diller D, Doweyko A, Sack J, Baldwin J, Barrish J, Dodd J, Henderson I, Kanner S, Schieven GL, Webb M. Leftheris K, et al. Among authors: schieven gl. J Med Chem. 2004 Dec 2;47(25):6283-91. doi: 10.1021/jm049521d. J Med Chem. 2004. PMID: 15566298
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: schieven gl. J Med Chem. 2004 Dec 30;47(27):6658-61. doi: 10.1021/jm049486a. J Med Chem. 2004. PMID: 15615512
109 results