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Page 1
The discovery of 6-amino nicotinamides as potent and selective histone deacetylase inhibitors.
Hamblett CL, Methot JL, Mampreian DM, Sloman DL, Stanton MG, Kral AM, Fleming JC, Cruz JC, Chenard M, Ozerova N, Hitz AM, Wang H, Deshmukh SV, Nazef N, Harsch A, Hughes B, Dahlberg WK, Szewczak AA, Middleton RE, Mosley RT, Secrist JP, Miller TA. Hamblett CL, et al. Among authors: szewczak aa. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5300-9. doi: 10.1016/j.bmcl.2007.08.023. Epub 2007 Aug 16. Bioorg Med Chem Lett. 2007. PMID: 17761416
Amino acid derivatives as histone deacetylase inhibitors.
Hubbs JL, Zhou H, Kral AM, Fleming JC, Dahlberg WK, Hughes BL, Middleton RE, Szewczak AA, Secrist JP, Miller TA. Hubbs JL, et al. Among authors: szewczak aa. Bioorg Med Chem Lett. 2008 Jan 1;18(1):34-8. doi: 10.1016/j.bmcl.2007.11.017. Epub 2007 Nov 13. Bioorg Med Chem Lett. 2008. PMID: 18042381
Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2).
Methot JL, Chakravarty PK, Chenard M, Close J, Cruz JC, Dahlberg WK, Fleming J, Hamblett CL, Hamill JE, Harrington P, Harsch A, Heidebrecht R, Hughes B, Jung J, Kenific CM, Kral AM, Meinke PT, Middleton RE, Ozerova N, Sloman DL, Stanton MG, Szewczak AA, Tyagarajan S, Witter DJ, Secrist JP, Miller TA. Methot JL, et al. Among authors: szewczak aa. Bioorg Med Chem Lett. 2008 Feb 1;18(3):973-8. doi: 10.1016/j.bmcl.2007.12.031. Epub 2008 Jan 7. Bioorg Med Chem Lett. 2008. PMID: 18182289
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
SAR profiles of spirocyclic nicotinamide derived selective HDAC1/HDAC2 inhibitors (SHI-1:2).
Methot JL, Hamblett CL, Mampreian DM, Jung J, Harsch A, Szewczak AA, Dahlberg WK, Middleton RE, Hughes B, Fleming JC, Wang H, Kral AM, Ozerova N, Cruz JC, Haines B, Chenard M, Kenific CM, Secrist JP, Miller TA. Methot JL, et al. Among authors: szewczak aa. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6104-9. doi: 10.1016/j.bmcl.2008.10.052. Epub 2008 Oct 14. Bioorg Med Chem Lett. 2008. PMID: 18951790
Parallel medicinal chemistry approaches to selective HDAC1/HDAC2 inhibitor (SHI-1:2) optimization.
Kattar SD, Surdi LM, Zabierek A, Methot JL, Middleton RE, Hughes B, Szewczak AA, Dahlberg WK, Kral AM, Ozerova N, Fleming JC, Wang H, Secrist P, Harsch A, Hamill JE, Cruz JC, Kenific CM, Chenard M, Miller TA, Berk SC, Tempest P. Kattar SD, et al. Among authors: szewczak aa. Bioorg Med Chem Lett. 2009 Feb 15;19(4):1168-72. doi: 10.1016/j.bmcl.2008.12.083. Epub 2008 Dec 25. Bioorg Med Chem Lett. 2009. PMID: 19138845
Exploring the pharmacokinetic properties of phosphorus-containing selective HDAC 1 and 2 inhibitors (SHI-1:2).
Heidebrecht RW Jr, Chenard M, Close J, Dahlberg WK, Fleming J, Grimm JB, Hamill JE, Harsch A, Haines BB, Hughes B, Kral AM, Middleton RE, Mushti C, Ozerova N, Szewczak AA, Wang H, Wilson K, Witter DJ, Secrist JP, Miller TA. Heidebrecht RW Jr, et al. Among authors: szewczak aa. Bioorg Med Chem Lett. 2009 Apr 1;19(7):2053-8. doi: 10.1016/j.bmcl.2009.02.009. Epub 2009 Feb 8. Bioorg Med Chem Lett. 2009. PMID: 19268585
Fluorinated piperidine acetic acids as gamma-secretase modulators.
Stanton MG, Hubbs J, Sloman D, Hamblett C, Andrade P, Angagaw M, Bi G, Black RM, Crispino J, Cruz JC, Fan E, Farris G, Hughes BL, Kenific CM, Middleton RE, Nikov G, Sajonz P, Shah S, Shomer N, Szewczak AA, Tanga F, Tudge MT, Shearman M, Munoz B. Stanton MG, et al. Among authors: szewczak aa. Bioorg Med Chem Lett. 2010 Jan 15;20(2):755-8. doi: 10.1016/j.bmcl.2009.11.034. Epub 2009 Nov 13. Bioorg Med Chem Lett. 2010. PMID: 20005099
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
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
42 results