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Page 1
The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases.
Tucker TJ, Abrams MT, Buser CA, Davide JP, Ellis-Hutchings M, Fernandes C, Gibbs JB, Graham SL, Hartman GD, Huber HE, Liu D, Lobell RB, Lumma WC, Robinson RG, Sisko JT, Smith AM. Tucker TJ, et al. Among authors: ellis hutchings m. Bioorg Med Chem Lett. 2002 Aug 5;12(15):2027-30. doi: 10.1016/s0960-894x(02)00308-6. Bioorg Med Chem Lett. 2002. PMID: 12113834
Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Nguyen DN, Stump CA, Walsh ES, Fernandes C, Davide JP, Ellis-Hutchings M, Robinson RG, Williams TM, Lobell RB, Huber HE, Buser CA. Nguyen DN, et al. Among authors: ellis hutchings m. Bioorg Med Chem Lett. 2002 May 6;12(9):1269-73. doi: 10.1016/s0960-894x(02)00154-3. Bioorg Med Chem Lett. 2002. PMID: 11965368
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: ellis hutchings m. J Med Chem. 2002 Jun 6;45(12):2388-409. doi: 10.1021/jm010531d. J Med Chem. 2002. PMID: 12036349
Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents.
deSolms SJ, Ciccarone TM, MacTough SC, Shaw AW, Buser CA, Ellis-Hutchings M, Fernandes C, Hamilton KA, Huber HE, Kohl NE, Lobell RB, Robinson RG, Tsou NN, Walsh ES, Graham SL, Beese LS, Taylor JS. deSolms SJ, et al. Among authors: ellis hutchings m. J Med Chem. 2003 Jul 3;46(14):2973-84. doi: 10.1021/jm020587n. J Med Chem. 2003. PMID: 12825937
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: ellis hutchings m. 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
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: ellis hutchings m. J Med Chem. 2001 Aug 30;44(18):2933-49. doi: 10.1021/jm010156p. J Med Chem. 2001. PMID: 11520202
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: ellis hutchings ms. 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
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: ellis hutchings ms. Cancer Res. 2001 Dec 15;61(24):8758-68. Cancer Res. 2001. PMID: 11751396