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Page 1
Diversity-oriented synthesis-facilitated medicinal chemistry: toward the development of novel antimalarial agents.
Comer E, Beaudoin JA, Kato N, Fitzgerald ME, Heidebrecht RW, Lee Md 4th, Masi D, Mercier M, Mulrooney C, Muncipinto G, Rowley A, Crespo-Llado K, Serrano AE, Lukens AK, Wiegand RC, Wirth DF, Palmer MA, Foley MA, Munoz B, Scherer CA, Duvall JR, Schreiber SL. Comer E, et al. Among authors: heidebrecht rw. J Med Chem. 2014 Oct 23;57(20):8496-502. doi: 10.1021/jm500994n. Epub 2014 Oct 13. J Med Chem. 2014. PMID: 25211597 Free PMC article.
Diversity-oriented synthesis probe targets Plasmodium falciparum cytochrome b ubiquinone reduction site and synergizes with oxidation site inhibitors.
Lukens AK, Heidebrecht RW Jr, Mulrooney C, Beaudoin JA, Comer E, Duvall JR, Fitzgerald ME, Masi D, Galinsky K, Scherer CA, Palmer M, Munoz B, Foley M, Schreiber SL, Wiegand RC, Wirth DF. Lukens AK, et al. Among authors: heidebrecht rw jr. J Infect Dis. 2015 Apr 1;211(7):1097-103. doi: 10.1093/infdis/jiu565. Epub 2014 Oct 21. J Infect Dis. 2015. PMID: 25336726 Free PMC article.
Diversity-Oriented Synthesis Yields a Novel Lead for the Treatment of Malaria.
Heidebrecht RW Jr, Mulrooney C, Austin CP, Barker RH Jr, Beaudoin JA, Cheng KC, Comer E, Dandapani S, Dick J, Duvall JR, Ekland EH, Fidock DA, Fitzgerald ME, Foley M, Guha R, Hinkson P, Kramer M, Lukens AK, Masi D, Marcaurelle LA, Su XZ, Thomas CJ, Weïwer M, Wiegand RC, Wirth D, Xia M, Yuan J, Zhao J, Palmer M, Munoz B, Schreiber S. Heidebrecht RW Jr, et al. ACS Med Chem Lett. 2012 Feb 9;3(2):112-117. doi: 10.1021/ml200244k. Epub 2011 Dec 22. ACS Med Chem Lett. 2012. PMID: 22328964 Free PMC article.
Delayed and Prolonged Histone Hyperacetylation with a Selective HDAC1/HDAC2 Inhibitor.
Methot JL, Hoffman DM, Witter DJ, Stanton MG, Harrington P, Hamblett C, Siliphaivanh P, Wilson K, Hubbs J, Heidebrecht R, Kral AM, Ozerova N, Fleming JC, Wang H, Szewczak AA, Middleton RE, Hughes B, Cruz JC, Haines BB, Chenard M, Kenific CM, Harsch A, Secrist JP, Miller TA. Methot JL, et al. ACS Med Chem Lett. 2014 Jan 2;5(4):340-5. doi: 10.1021/ml4004233. eCollection 2014 Apr 10. ACS Med Chem Lett. 2014. PMID: 24900838 Free PMC article.
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. 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
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. 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
Divergent kinetics differentiate the mechanism of action of two HDAC inhibitors.
Kral AM, Ozerova N, Close J, Jung J, Chenard M, Fleming J, Haines BB, Harrington P, Maclean J, Miller TA, Secrist P, Wang H, Heidebrecht RW Jr. Kral AM, et al. Among authors: heidebrecht rw jr. Biochemistry. 2014 Feb 4;53(4):725-34. doi: 10.1021/bi400936h. Epub 2014 Jan 22. Biochemistry. 2014. PMID: 24450491
Lead optimization of 4,4-biaryl piperidine amides as γ-secretase inhibitors.
Close J, Heidebrecht R Jr, Hendrix J, Li C, Munoz B, Surdi L, Kattar S, Tempest P, Moses P, Geng X, Hughes B, Smotrov N, Moxham C, Chapnick J, Kariv I, Nikov G, Burke JE, Deshmukh S, Jeliazkova-Mecheva V, Leach JK, Diaz D, Xu L, Yang Z, Kwei G, Moy L, Shah S, Tanga F, Kenefic C, Savage D, Shearman M, Ball RG, McNevin MJ, Markarewicz A, Miller T. Close J, et al. Bioorg Med Chem Lett. 2012 May 1;22(9):3203-7. doi: 10.1016/j.bmcl.2012.03.038. Epub 2012 Mar 17. Bioorg Med Chem Lett. 2012. PMID: 22483609
14 results