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A Brain Penetrant Mutant IDH1 Inhibitor Provides In Vivo Survival Benefit.
Kopinja J, Sevilla RS, Levitan D, Dai D, Vanko A, Spooner E, Ware C, Forget R, Hu K, Kral A, Spacciapoli P, Kennan R, Jayaraman L, Pucci V, Perera S, Zhang W, Fischer C, Lam MH. Kopinja J, et al. Among authors: kral a. Sci Rep. 2017 Oct 23;7(1):13853. doi: 10.1038/s41598-017-14065-w. Sci Rep. 2017. PMID: 29062039 Free PMC article.
Evaluation of farnesyl:protein transferase and geranylgeranyl:protein transferase inhibitor combinations in preclinical models.
Lobell RB, Omer CA, Abrams MT, Bhimnathwala HG, Brucker MJ, Buser CA, Davide JP, deSolms SJ, Dinsmore CJ, Ellis-Hutchings MS, Kral AM, Liu D, Lumma WC, Machotka SV, Rands E, Williams TM, Graham SL, Hartman GD, Oliff AI, Heimbrook DC, Kohl NE. Lobell RB, et al. Among authors: kral am. Cancer Res. 2001 Dec 15;61(24):8758-68. Cancer Res. 2001. PMID: 11751396
An Unbiased Oncology Compound Screen to Identify Novel Combination Strategies.
O'Neil J, Benita Y, Feldman I, Chenard M, Roberts B, Liu Y, Li J, Kral A, Lejnine S, Loboda A, Arthur W, Cristescu R, Haines BB, Winter C, Zhang T, Bloecher A, Shumway SD. O'Neil J, et al. Among authors: kral a. Mol Cancer Ther. 2016 Jun;15(6):1155-62. doi: 10.1158/1535-7163.MCT-15-0843. Epub 2016 Mar 16. Mol Cancer Ther. 2016. PMID: 26983881
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: kral am. 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
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: kral am. 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
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
Witter DJ, Harrington P, Wilson KJ, Chenard M, Fleming JC, Haines B, Kral AM, Secrist JP, Miller TA. Witter DJ, et al. Among authors: kral am. Bioorg Med Chem Lett. 2008 Jan 15;18(2):726-31. doi: 10.1016/j.bmcl.2007.11.047. Epub 2007 Nov 19. Bioorg Med Chem Lett. 2008. PMID: 18060775
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: kral am. 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
474 results