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Page 1
Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met.
Northrup AB, Katcher MH, Altman MD, Chenard M, Daniels MH, Deshmukh SV, Falcone D, Guerin DJ, Hatch H, Li C, Lu W, Lutterbach B, Allison TJ, Patel SB, Reilly JF, Reutershan M, Rickert KW, Rosenstein C, Soisson SM, Szewczak AA, Walker D, Wilson K, Young JR, Pan BS, Dinsmore CJ. Northrup AB, et al. Among authors: szewczak aa. J Med Chem. 2013 Mar 28;56(6):2294-310. doi: 10.1021/jm301619u. Epub 2013 Mar 18. J Med Chem. 2013. PMID: 23379595
MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.
Pan BS, Chan GK, Chenard M, Chi A, Davis LJ, Deshmukh SV, Gibbs JB, Gil S, Hang G, Hatch H, Jewell JP, Kariv I, Katz JD, Kunii K, Lu W, Lutterbach BA, Paweletz CP, Qu X, Reilly JF, Szewczak AA, Zeng Q, Kohl NE, Dinsmore CJ. Pan BS, et al. Among authors: szewczak aa. Cancer Res. 2010 Feb 15;70(4):1524-33. doi: 10.1158/0008-5472.CAN-09-2541. Epub 2010 Feb 9. Cancer Res. 2010. PMID: 20145145
Genetic and pharmacological inhibition of PDK1 in cancer cells: characterization of a selective allosteric kinase inhibitor.
Nagashima K, Shumway SD, Sathyanarayanan S, Chen AH, Dolinski B, Xu Y, Keilhack H, Nguyen T, Wiznerowicz M, Li L, Lutterbach BA, Chi A, Paweletz C, Allison T, Yan Y, Munshi SK, Klippel A, Kraus M, Bobkova EV, Deshmukh S, Xu Z, Mueller U, Szewczak AA, Pan BS, Richon V, Pollock R, Blume-Jensen P, Northrup A, Andersen JN. Nagashima K, et al. Among authors: szewczak aa. J Biol Chem. 2011 Feb 25;286(8):6433-48. doi: 10.1074/jbc.M110.156463. Epub 2010 Nov 30. J Biol Chem. 2011. PMID: 21118801 Free PMC article.
Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.
Katz JD, Jewell JP, Guerin DJ, Lim J, Dinsmore CJ, Deshmukh SV, Pan BS, Marshall CG, Lu W, Altman MD, Dahlberg WK, Davis L, Falcone D, Gabarda AE, Hang G, Hatch H, Holmes R, Kunii K, Lumb KJ, Lutterbach B, Mathvink R, Nazef N, Patel SB, Qu X, Reilly JF, Rickert KW, Rosenstein C, Soisson SM, Spencer KB, Szewczak AA, Walker D, Wang W, Young J, Zeng Q. Katz JD, et al. Among authors: szewczak aa. J Med Chem. 2011 Jun 23;54(12):4092-108. doi: 10.1021/jm200112k. Epub 2011 May 24. J Med Chem. 2011. PMID: 21608528
Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.
Lim J, Taoka B, Otte RD, Spencer K, Dinsmore CJ, Altman MD, Chan G, Rosenstein C, Sharma S, Su HP, Szewczak AA, Xu L, Yin H, Zugay-Murphy J, Marshall CG, Young JR. Lim J, et al. Among authors: szewczak aa. J Med Chem. 2011 Oct 27;54(20):7334-49. doi: 10.1021/jm200909u. Epub 2011 Sep 26. J Med Chem. 2011. PMID: 21942426
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.
Katz JD, Haidle A, Childers KK, Zabierek AA, Jewell JP, Hou Y, Altman MD, Szewczak A, Chen D, Harsch A, Hayashi M, Warren L, Hutton M, Nuthall H, Su HP, Munshi S, Stanton MG, Davies IW, Munoz B, Northrup A. Katz JD, et al. Among authors: szewczak a. Bioorg Med Chem Lett. 2017 Jan 1;27(1):114-120. doi: 10.1016/j.bmcl.2016.08.068. Epub 2016 Oct 22. Bioorg Med Chem Lett. 2017. PMID: 27816515
MARK inhibitors: Declaring a No-Go decision on a chemical series based on extensive DMPK experimentation.
Haidle AM, Childers KK, Zabierek AA, Katz JD, Jewell JP, Hou Y, Altman MD, Szewczak A, Chen D, Harsch A, Hayashi M, Warren L, Hutton M, Nuthall H, Stanton MG, Davies IW, Munoz B, Northrup A. Haidle AM, et al. Among authors: szewczak a. Bioorg Med Chem Lett. 2017 Jan 1;27(1):109-113. doi: 10.1016/j.bmcl.2016.08.066. Epub 2016 Aug 25. Bioorg Med Chem Lett. 2017. PMID: 27894874
Phenylglycine and phenylalanine derivatives as potent and selective HDAC1 inhibitors (SHI-1).
Wilson KJ, Witter DJ, Grimm JB, Siliphaivanh P, Otte KM, Kral AM, Fleming JC, Harsch A, Hamill JE, Cruz JC, Chenard M, Szewczak AA, Middleton RE, Hughes BL, Dahlberg WK, Secrist JP, Miller TA. Wilson KJ, et al. Among authors: szewczak aa. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1859-63. doi: 10.1016/j.bmcl.2008.02.012. Epub 2008 Feb 10. Bioorg Med Chem Lett. 2008. PMID: 18304810
Purine derivatives as potent gamma-secretase modulators.
Rivkin A, Ahearn SP, Chichetti SM, Hamblett CL, Garcia Y, Martinez M, Hubbs JL, Reutershan MH, Daniels MH, Siliphaivanh P, Otte KM, Li C, Rosenau A, Surdi LM, Jung J, Hughes BL, Crispino JL, Nikov GN, Middleton RE, Moxham CM, Szewczak AA, Shah S, Moy LY, Kenific CM, Tanga F, Cruz JC, Andrade P, Angagaw MH, Shomer NH, Miller T, Munoz B, Shearman MS. Rivkin A, et al. Among authors: szewczak aa. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2279-82. doi: 10.1016/j.bmcl.2010.02.008. Epub 2010 Feb 6. Bioorg Med Chem Lett. 2010. PMID: 20207146
42 results