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Page 1
From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: the discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis.
Santella JB 3rd, Gardner DS, Yao W, Shi C, Reddy P, Tebben AJ, DeLucca GV, Wacker DA, Watson PS, Welch PK, Wadman EA, Davies P, Solomon KA, Graden DM, Yeleswaram S, Mandlekar S, Kariv I, Decicco CP, Ko SS, Carter PH, Duncia JV. Santella JB 3rd, et al. Among authors: carter ph. Bioorg Med Chem Lett. 2008 Jan 15;18(2):576-85. doi: 10.1016/j.bmcl.2007.11.067. Epub 2007 Nov 22. Bioorg Med Chem Lett. 2008. PMID: 18096386
Photochemically enhanced binding of small molecules to the tumor necrosis factor receptor-1 inhibits the binding of TNF-alpha.
Carter PH, Scherle PA, Muckelbauer JK, Voss ME, Liu RQ, Thompson LA, Tebben AJ, Solomon KA, Lo YC, Li Z, Strzemienski P, Yang G, Falahatpisheh N, Xu M, Wu Z, Farrow NA, Ramnarayan K, Wang J, Rideout D, Yalamoori V, Domaille P, Underwood DJ, Trzaskos JM, Friedman SM, Newton RC, Decicco CP. Carter PH, et al. Proc Natl Acad Sci U S A. 2001 Oct 9;98(21):11879-84. doi: 10.1073/pnas.211178398. Proc Natl Acad Sci U S A. 2001. PMID: 11592999 Free PMC article.
Both 5-arylidene-2-thioxodihydropyrimidine-4,6(1H,5H)-diones and 3-thioxo-2,3-dihydro-1H-imidazo[1,5-a]indol-1-ones are light-dependent tumor necrosis factor-alpha antagonists.
Voss ME, Carter PH, Tebben AJ, Scherle PA, Brown GD, Thompson LA, Xu M, Lo YC, Yang G, Liu RQ, Strzemienski P, Everlof JG, Trzaskos JM, Decicco CP. Voss ME, et al. Among authors: carter ph. Bioorg Med Chem Lett. 2003 Feb 10;13(3):533-8. doi: 10.1016/s0960-894x(02)00941-1. Bioorg Med Chem Lett. 2003. PMID: 12565966
N-Arylalkylpiperidine urea derivatives as CC chemokine receptor-3 (CCR3) antagonists.
Batt DG, Houghton GC, Roderick J, Santella JB 3rd, Wacker DA, Welch PK, Orlovsky YI, Wadman EA, Trzaskos JM, Davies P, Decicco CP, Carter PH. Batt DG, et al. Among authors: carter ph. Bioorg Med Chem Lett. 2005 Feb 1;15(3):787-91. doi: 10.1016/j.bmcl.2004.11.006. Bioorg Med Chem Lett. 2005. PMID: 15664858
Selective inhibition of eosinophil influx into the lung by small molecule CC chemokine receptor 3 antagonists in mouse models of allergic inflammation.
Das AM, Vaddi KG, Solomon KA, Krauthauser C, Jiang X, McIntyre KW, Yang XX, Wadman E, Welch P, Covington M, Graden D, Yeleswaram K, Trzaskos JM, Newton RC, Mandlekar S, Ko SS, Carter PH, Davies P. Das AM, et al. Among authors: carter ph. J Pharmacol Exp Ther. 2006 Jul;318(1):411-7. doi: 10.1124/jpet.105.099812. Epub 2006 Apr 13. J Pharmacol Exp Ther. 2006. PMID: 16614169
CC chemokine receptor-3 (CCR3) antagonists: improving the selectivity of DPC168 by reducing central ring lipophilicity.
Pruitt JR, Batt DG, Wacker DA, Bostrom LL, Booker SK, McLaughlin E, Houghton GC, Varnes JG, Christ DD, Covington M, Das AM, Davies P, Graden D, Kariv I, Orlovsky Y, Stowell NC, Vaddi KG, Wadman EA, Welch PK, Yeleswaram S, Solomon KA, Newton RC, Decicco CP, Carter PH, Ko SS. Pruitt JR, et al. Among authors: carter ph. Bioorg Med Chem Lett. 2007 Jun 1;17(11):2992-7. doi: 10.1016/j.bmcl.2007.03.065. Epub 2007 Mar 24. Bioorg Med Chem Lett. 2007. PMID: 17418570
Discovery of a small molecule antagonist of the parathyroid hormone receptor by using an N-terminal parathyroid hormone peptide probe.
Carter PH, Liu RQ, Foster WR, Tamasi JA, Tebben AJ, Favata M, Staal A, Cvijic ME, French MH, Dell V, Apanovitch D, Lei M, Zhao Q, Cunningham M, Decicco CP, Trzaskos JM, Feyen JH. Carter PH, et al. Proc Natl Acad Sci U S A. 2007 Apr 17;104(16):6846-51. doi: 10.1073/pnas.0605125104. Epub 2007 Apr 11. Proc Natl Acad Sci U S A. 2007. PMID: 17428923 Free PMC article.
From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part II: Acyclic replacements for the (3S)-3-benzylpiperidine in a series of potent CCR3 antagonists.
Gardner DS, Santella JB 3rd, Tebben AJ, Batt DG, Ko SS, Traeger SC, Welch PK, Wadman EA, Davies P, Carter PH, Duncia JV. Gardner DS, et al. Among authors: carter ph. Bioorg Med Chem Lett. 2008 Jan 15;18(2):586-95. doi: 10.1016/j.bmcl.2007.11.087. Epub 2007 Nov 28. Bioorg Med Chem Lett. 2008. PMID: 18160284
112 results