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Page 1
N-arylpiperazinone inhibitors of farnesyltransferase: discovery and biological activity.
Williams TM, Bergman JM, Brashear K, Breslin MJ, Dinsmore CJ, Hutchinson JH, MacTough SC, Stump CA, Wei DD, Zartman CB, Bogusky MJ, Culberson JC, Buser-Doepner C, Davide J, Greenberg IB, Hamilton KA, Koblan KS, Kohl NE, Liu D, Lobell RB, Mosser SD, O'Neill TJ, Rands E, Schaber MD, Huff JR, et al. Williams TM, et al. Among authors: culberson jc. J Med Chem. 1999 Sep 23;42(19):3779-84. doi: 10.1021/jm990254z. J Med Chem. 1999. PMID: 10508426 No abstract available.
3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.
Bell IM, Gallicchio SN, Abrams M, Beese LS, Beshore DC, Bhimnathwala H, Bogusky MJ, Buser CA, Culberson JC, Davide J, Ellis-Hutchings M, Fernandes C, Gibbs JB, Graham SL, Hamilton KA, Hartman GD, Heimbrook DC, Homnick CF, Huber HE, Huff JR, Kassahun K, Koblan KS, Kohl NE, Lobell RB, Lynch JJ Jr, Robinson R, Rodrigues AD, Taylor JS, Walsh ES, Williams TM, Zartman CB. Bell IM, et al. Among authors: culberson jc. J Med Chem. 2002 Jun 6;45(12):2388-409. doi: 10.1021/jm010531d. J Med Chem. 2002. PMID: 12036349
Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Dinsmore CJ, Zartman CB, Bergman JM, Abrams MT, Buser CA, Culberson JC, Davide JP, Ellis-Hutchings M, Fernandes C, Graham SL, Hartman GD, Huber HE, Lobell RB, Mosser SD, Robinson RG, Williams TM. Dinsmore CJ, et al. Among authors: culberson jc. Bioorg Med Chem Lett. 2004 Feb 9;14(3):639-43. doi: 10.1016/j.bmcl.2003.11.051. Bioorg Med Chem Lett. 2004. PMID: 14741259
Non-thiol 3-aminomethylbenzamide inhibitors of farnesyl-protein transferase.
Ciccarone TM, MacTough SC, Williams TM, Dinsmore CJ, O'Neill TJ, Shah D, Culberson JC, Koblan KS, Kohl NE, Gibbs JB, Oliff AI, Graham SL, Hartman GD. Ciccarone TM, et al. Among authors: culberson jc. Bioorg Med Chem Lett. 1999 Jul 19;9(14):1991-6. doi: 10.1016/s0960-894x(99)00323-6. Bioorg Med Chem Lett. 1999. PMID: 10450968
Evaluation of amino acid-based linkers in potent macrocyclic inhibitors of farnesyl-protein transferase.
Beshore DC, Bell IM, Dinsmore CJ, Homnick CF, Culberson JC, Robinson RG, Fernandes C, Walsh ES, Abrams MT, Bhimnathwala HG, Davide JP, Ellis-Hutchings MS, Huber HA, Koblan KS, Buser CA, Kohl NE, Lobell RB, Chen IW, McLoughlin DA, Olah TV, Graham SL, Hartman GD, Williams TM. Beshore DC, et al. Among authors: culberson jc. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1817-21. doi: 10.1016/s0960-894x(01)00340-7. Bioorg Med Chem Lett. 2001. PMID: 11459639
Design and biological activity of (S)-4-(5-([1-(3-chlorobenzyl)-2-oxopyrrolidin-3-ylamino]methyl)imidazol-1-ylmethyl)benzonitrile, a 3-aminopyrrolidinone farnesyltransferase inhibitor with excellent cell potency.
Bell IM, Gallicchio SN, Abrams M, Beshore DC, Buser CA, Culberson JC, Davide J, Ellis-Hutchings M, Fernandes C, Gibbs JB, Graham SL, Hartman GD, Heimbrook DC, Homnick CF, Huff JR, Kassahun K, Koblan KS, Kohl NE, Lobell RB, Lynch JJ Jr, Miller PA, Omer CA, Rodrigues AD, Walsh ES, Williams TM. Bell IM, et al. Among authors: culberson jc. J Med Chem. 2001 Aug 30;44(18):2933-49. doi: 10.1021/jm010156p. J Med Chem. 2001. PMID: 11520202
NMR studies of novel inhibitors bound to farnesyl-protein transferase.
Koblan KS, Culberson JC, Desolms SJ, Giuliani EA, Mosser SD, Omer CA, Pitzenberger SM, Bogusky MJ. Koblan KS, et al. Among authors: culberson jc. Protein Sci. 1995 Apr;4(4):681-8. doi: 10.1002/pro.5560040408. Protein Sci. 1995. PMID: 7613466 Free PMC article.
45 results