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Page 1
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: gallicchio sn. J Med Chem. 2002 Jun 6;45(12):2388-409. doi: 10.1021/jm010531d. J Med Chem. 2002. PMID: 12036349
Development of orally active oxytocin antagonists: studies on 1-(1-[4-[1-(2-methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2- methoxybenzoyl]piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and related pyridines.
Bell IM, Erb JM, Freidinger RM, Gallicchio SN, Guare JP, Guidotti MT, Halpin RA, Hobbs DW, Homnick CF, Kuo MS, Lis EV, Mathre DJ, Michelson SR, Pawluczyk JM, Pettibone DJ, Reiss DR, Vickers S, Williams PD, Woyden CJ. Bell IM, et al. Among authors: gallicchio sn. J Med Chem. 1998 Jun 4;41(12):2146-63. doi: 10.1021/jm9800797. J Med Chem. 1998. PMID: 9622556
Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.
Williams PD, Bock MG, Evans BE, Freidinger RM, Gallicchio SN, Guidotti MT, Jacobson MA, Kuo MS, Levy MR, Lis EV, Michelson SR, Pawluczyk JM, Perlow DS, Pettibone DJ, Quigley AG, Reiss DR, Salvatore C, Stauffer KJ, Woyden CJ. Williams PD, et al. Among authors: gallicchio sn. Bioorg Med Chem Lett. 1999 May 3;9(9):1311-6. doi: 10.1016/s0960-894x(99)00181-x. Bioorg Med Chem Lett. 1999. PMID: 10340620
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: gallicchio sn. J Med Chem. 2001 Aug 30;44(18):2933-49. doi: 10.1021/jm010156p. J Med Chem. 2001. PMID: 11520202
Biochemical and structural characterization of a novel class of inhibitors of the type 1 insulin-like growth factor and insulin receptor kinases.
Bell IM, Stirdivant SM, Ahern J, Culberson JC, Darke PL, Dinsmore CJ, Drakas RA, Gallicchio SN, Graham SL, Heimbrook DC, Hall DL, Hua J, Kett NR, Kim AS, Kornienko M, Kuo LC, Munshi SK, Quigley AG, Reid JC, Trotter BW, Waxman LH, Williams TM, Zartman CB. Bell IM, et al. Among authors: gallicchio sn. Biochemistry. 2005 Jul 12;44(27):9430-40. doi: 10.1021/bi0500628. Biochemistry. 2005. PMID: 15996097
Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead.
Williams TM, Stump CA, Nguyen DN, Quigley AG, Bell IM, Gallicchio SN, Zartman CB, Wan BL, Penna KD, Kunapuli P, Kane SA, Koblan KS, Mosser SD, Rutledge RZ, Salvatore C, Fay JF, Vacca JP, Graham SL. Williams TM, et al. Among authors: gallicchio sn. Bioorg Med Chem Lett. 2006 May 15;16(10):2595-8. doi: 10.1016/j.bmcl.2006.02.051. Epub 2006 Mar 9. Bioorg Med Chem Lett. 2006. PMID: 16527483
Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists.
Bell IM, Bednar RA, Fay JF, Gallicchio SN, Hochman JH, McMasters DR, Miller-Stein C, Moore EL, Mosser SD, Pudvah NT, Quigley AG, Salvatore CA, Stump CA, Theberge CR, Wong BK, Zartman CB, Zhang XF, Kane SA, Graham SL, Vacca JP, Williams TM. Bell IM, et al. Among authors: gallicchio sn. Bioorg Med Chem Lett. 2006 Dec 15;16(24):6165-9. doi: 10.1016/j.bmcl.2006.09.045. Epub 2006 Oct 5. Bioorg Med Chem Lett. 2006. PMID: 17027263
The discovery of highly potent CGRP receptor antagonists.
Stump CA, Bell IM, Bednar RA, Bruno JG, Fay JF, Gallicchio SN, Johnston VK, Moore EL, Mosser SD, Quigley AG, Salvatore CA, Theberge CR, Blair Zartman C, Zhang XF, Kane SA, Graham SL, Vacca JP, Williams TM. Stump CA, et al. Among authors: gallicchio sn. Bioorg Med Chem Lett. 2009 Jan 1;19(1):214-7. doi: 10.1016/j.bmcl.2008.10.106. Epub 2008 Oct 31. Bioorg Med Chem Lett. 2009. PMID: 19010673
The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists.
Bell IM, Bednar RA, Corcoran HA, Fay JF, Gallicchio SN, Johnston VK, Hershey JC, Miller-Stein CM, Moore EL, Mosser SD, Roller SA, Salvatore CA, Theberge CR, Wong BK, Blair Zartman C, Kane SA, Williams TM, Graham SL, Vacca JP. Bell IM, et al. Among authors: gallicchio sn. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4740-2. doi: 10.1016/j.bmcl.2009.06.057. Epub 2009 Jun 17. Bioorg Med Chem Lett. 2009. PMID: 19577468
Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist.
Salvatore CA, Moore EL, Calamari A, Cook JJ, Michener MS, O'Malley S, Miller PJ, Sur C, Williams DL Jr, Zeng Z, Danziger A, Lynch JJ, Regan CP, Fay JF, Tang YS, Li CC, Pudvah NT, White RB, Bell IM, Gallicchio SN, Graham SL, Selnick HG, Vacca JP, Kane SA. Salvatore CA, et al. Among authors: gallicchio sn. J Pharmacol Exp Ther. 2010 Apr;333(1):152-60. doi: 10.1124/jpet.109.163816. Epub 2010 Jan 11. J Pharmacol Exp Ther. 2010. PMID: 20065019
18 results