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Page 1
2-Arylindole-3-acetamides: FPP-competitive inhibitors of farnesyl protein transferase.
Trotter BW, Quigley AG, Lumma WC, Sisko JT, Walsh ES, Hamann CS, Robinson RG, Bhimnathwala H, Kolodin DG, Zheng W, Buser CA, Huber HE, Lobell RB, Kohl NE, Williams TM, Graham SL, Dinsmore CJ. Trotter BW, et al. Among authors: lumma wc. Bioorg Med Chem Lett. 2001 Apr 9;11(7):865-9. doi: 10.1016/s0960-894x(01)00061-0. Bioorg Med Chem Lett. 2001. PMID: 11294379
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: lumma wc. 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
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: lumma wc. Cancer Res. 2001 Dec 15;61(24):8758-68. Cancer Res. 2001. PMID: 11751396
Anions modulate the potency of geranylgeranyl-protein transferase I inhibitors.
Huber HE, Robinson RG, Watkins A, Nahas DD, Abrams MT, Buser CA, Lobell RB, Patrick D, Anthony NJ, Dinsmore CJ, Graham SL, Hartman GD, Lumma WC, Williams TM, Heimbrook DC. Huber HE, et al. Among authors: lumma wc. J Biol Chem. 2001 Jul 6;276(27):24457-65. doi: 10.1074/jbc.M100325200. Epub 2001 Mar 26. J Biol Chem. 2001. PMID: 11274181 Free article.
Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position.
Tucker TJ, Lumma WC, Lewis SD, Gardell SJ, Lucas BJ, Sisko JT, Lynch JJ, Lyle EA, Baskin EP, Woltmann RF, Appleby SD, Chen IW, Dancheck KB, Naylor-Olsen AM, Krueger JA, Cooper CM, Vacca JP. Tucker TJ, et al. Among authors: lumma wc. J Med Chem. 1997 Oct 24;40(22):3687-93. doi: 10.1021/jm970397q. J Med Chem. 1997. PMID: 9357536
Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.
Tucker TJ, Brady SF, Lumma WC, Lewis SD, Gardell SJ, Naylor-Olsen AM, Yan Y, Sisko JT, Stauffer KJ, Lucas BJ, Lynch JJ, Cook JJ, Stranieri MT, Holahan MA, Lyle EA, Baskin EP, Chen IW, Dancheck KB, Krueger JA, Cooper CM, Vacca JP. Tucker TJ, et al. Among authors: lumma wc. J Med Chem. 1998 Aug 13;41(17):3210-9. doi: 10.1021/jm9801713. J Med Chem. 1998. PMID: 9703466
Potent noncovalent thrombin inhibitors that utilize the unique amino acid D-dicyclohexylalanine in the P3 position. Implications on oral bioavailability and antithrombotic efficacy.
Tucker TJ, Lumma WC, Lewis SD, Gardell SJ, Lucas BJ, Baskin EP, Woltmann R, Lynch JJ, Lyle EA, Appleby SD, Chen IW, Dancheck KB, Vacca JP. Tucker TJ, et al. Among authors: lumma wc. J Med Chem. 1997 May 23;40(11):1565-9. doi: 10.1021/jm970140s. J Med Chem. 1997. PMID: 9171866
37 results