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47 results

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Page 1
The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode.
Wrobleski ST, Lin S, Dhar TG, Dyckman AJ, Li T, Pitt S, Zhang R, Fan Y, Doweyko AM, Tokarski JS, Kish KF, Kiefer SE, Sack JS, Newitt JA, Witmer MR, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K. Wrobleski ST, et al. Among authors: leftheris k. Bioorg Med Chem Lett. 2013 Jul 15;23(14):4120-6. doi: 10.1016/j.bmcl.2013.05.047. Epub 2013 May 23. Bioorg Med Chem Lett. 2013. PMID: 23746475
Discovery and structure-activity relationships of imidazole-containing tetrahydrobenzodiazepine inhibitors of farnesyltransferase.
Ding CZ, Batorsky R, Bhide R, Chao HJ, Cho Y, Chong S, Gullo-Brown J, Guo P, Kim SH, Lee F, Leftheris K, Miller A, Mitt T, Patel M, Penhallow BA, Ricca C, Rose WC, Schmidt R, Slusarchyk WA, Vite G, Yan N, Manne V, Hunt JT. Ding CZ, et al. Among authors: leftheris k. J Med Chem. 1999 Dec 16;42(25):5241-53. doi: 10.1021/jm990391w. J Med Chem. 1999. PMID: 10602709
Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity.
Hunt JT, Ding CZ, Batorsky R, Bednarz M, Bhide R, Cho Y, Chong S, Chao S, Gullo-Brown J, Guo P, Kim SH, Lee FY, Leftheris K, Miller A, Mitt T, Patel M, Penhallow BA, Ricca C, Rose WC, Schmidt R, Slusarchyk WA, Vite G, Manne V. Hunt JT, et al. Among authors: leftheris k. J Med Chem. 2000 Oct 5;43(20):3587-95. doi: 10.1021/jm000248z. J Med Chem. 2000. PMID: 11020273
C-3 Amido-indole cannabinoid receptor modulators.
Hynes J Jr, Leftheris K, Wu H, Pandit C, Chen P, Norris DJ, Chen BC, Zhao R, Kiener PA, Chen X, Turk LA, Patil-Koota V, Gillooly KM, Shuster DJ, McIntyre KW. Hynes J Jr, et al. Among authors: leftheris k. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2399-402. doi: 10.1016/s0960-894x(02)00466-3. Bioorg Med Chem Lett. 2002. PMID: 12161142
Novel guanidine-based inhibitors of inosine monophosphate dehydrogenase.
Iwanowicz EJ, Watterson SH, Liu C, Gu HH, Mitt T, Leftheris K, Barrish JC, Fleener CA, Rouleau K, Sherbina NZ, Hollenbaugh DL. Iwanowicz EJ, et al. Among authors: leftheris k. Bioorg Med Chem Lett. 2002 Oct 21;12(20):2931-4. doi: 10.1016/s0960-894x(02)00600-5. Bioorg Med Chem Lett. 2002. PMID: 12270177
Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties.
Wrobleski ST, Chen P, Hynes J Jr, Lin S, Norris DJ, Pandit CR, Spergel S, Wu H, Tokarski JS, Chen X, Gillooly KM, Kiener PA, McIntyre KW, Patil-Koota V, Shuster DJ, Turk LA, Yang G, Leftheris K. Wrobleski ST, et al. Among authors: leftheris k. J Med Chem. 2003 May 22;46(11):2110-6. doi: 10.1021/jm020329q. J Med Chem. 2003. PMID: 12747783
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).
Pitts WJ, Vaccaro W, Huynh T, Leftheris K, Roberge JY, Barbosa J, Guo J, Brown B, Watson A, Donaldson K, Starling GC, Kiener PA, Poss MA, Dodd JH, Barrish JC. Pitts WJ, et al. Among authors: leftheris k. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2955-8. doi: 10.1016/j.bmcl.2004.03.021. Bioorg Med Chem Lett. 2004. PMID: 15125967
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. J Med Chem. 2004 Dec 2;47(25):6283-91. doi: 10.1021/jm049521d. J Med Chem. 2004. PMID: 15566298
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: leftheris k. J Med Chem. 2005 Oct 6;48(20):6261-70. doi: 10.1021/jm0503594. J Med Chem. 2005. PMID: 16190753
47 results