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260 results

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Page 1
Utilization of a nitrogen-sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase inhibitors.
Lin S, Wrobleski ST, Hynes J Jr, Pitt S, Zhang R, Fan Y, Doweyko AM, Kish KF, Sack JS, Malley MF, Kiefer SE, Newitt JA, McKinnon M, Trzaskos J, Barrish JC, Dodd JH, Schieven GL, Leftheris K. Lin S, et al. Among authors: pitt s. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5864-8. doi: 10.1016/j.bmcl.2010.07.102. Epub 2010 Jul 30. Bioorg Med Chem Lett. 2010. PMID: 20732813
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: pitt s. 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 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: pitt s. 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: pitt s. 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: pitt s. J Med Chem. 2004 Dec 30;47(27):6658-61. doi: 10.1021/jm049486a. J Med Chem. 2004. PMID: 15615512
5-Cyanopyrimidine derivatives as a novel class of potent, selective, and orally active inhibitors of p38alpha MAP kinase.
Liu C, Wrobleski ST, Lin J, Ahmed G, Metzger A, Wityak J, Gillooly KM, Shuster DJ, McIntyre KW, Pitt S, Shen DR, Zhang RF, Zhang H, Doweyko AM, Diller D, Henderson I, Barrish JC, Dodd JH, Schieven GL, Leftheris K. Liu C, et al. Among authors: pitt s. J Med Chem. 2005 Oct 6;48(20):6261-70. doi: 10.1021/jm0503594. J Med Chem. 2005. PMID: 16190753
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: pitt s. J Med Chem. 2006 Nov 16;49(23):6819-32. doi: 10.1021/jm060727j. J Med Chem. 2006. PMID: 17154512
260 results