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Page 1
Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency.
De Lucca GV, Kim UT, Vargo BJ, Duncia JV, Santella JB 3rd, Gardner DS, Zheng C, Liauw A, Wang Z, Emmett G, Wacker DA, Welch PK, Covington M, Stowell NC, Wadman EA, Das AM, Davies P, Yeleswaram S, Graden DM, Solomon KA, Newton RC, Trainor GL, Decicco CP, Ko SS. De Lucca GV, et al. Among authors: duncia jv. J Med Chem. 2005 Mar 24;48(6):2194-211. doi: 10.1021/jm049530m. J Med Chem. 2005. PMID: 15771462
CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure-activity relationships.
Wacker DA, Santella JB 3rd, Gardner DS, Varnes JG, Estrella M, DeLucca GV, Ko SS, Tanabe K, Watson PS, Welch PK, Covington M, Stowell NC, Wadman EA, Davies P, Solomon KA, Newton RC, Trainor GL, Friedman SM, Decicco CP, Duncia JV. Wacker DA, et al. Among authors: duncia jv. Bioorg Med Chem Lett. 2002 Jul 8;12(13):1785-9. doi: 10.1016/s0960-894x(02)00206-8. Bioorg Med Chem Lett. 2002. PMID: 12067561
Discovery of N-propylurea 3-benzylpiperidines as selective CC chemokine receptor-3 (CCR3) antagonists.
Varnes JG, Gardner DS, Santella JB 3rd, Duncia JV, Estrella M, Watson PS, Clark CM, Ko SS, Welch P, Covington M, Stowell N, Wadman E, Davies P, Solomon K, Newton RC, Trainor GL, Decicco CP, Wacker DA. Varnes JG, et al. Among authors: duncia jv. Bioorg Med Chem Lett. 2004 Apr 5;14(7):1645-9. doi: 10.1016/j.bmcl.2004.01.059. Bioorg Med Chem Lett. 2004. PMID: 15026042
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: duncia jv. 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
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: duncia jv. 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
gamma-Lactams as glycinamide replacements in cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists.
Cherney RJ, Mo R, Meyer DT, Voss ME, Yang MG, Santella JB 3rd, Duncia JV, Lo YC, Yang G, Miller PB, Scherle PA, Zhao Q, Mandlekar S, Cvijic ME, Barrish JC, Decicco CP, Carter PH. Cherney RJ, et al. Among authors: duncia jv. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2425-30. doi: 10.1016/j.bmcl.2010.03.035. Epub 2010 Mar 10. Bioorg Med Chem Lett. 2010. PMID: 20346664
The discovery of BMS-457, a potent and selective CCR1 antagonist.
Gardner DS, Santella JB 3rd, Duncia JV, Carter PH, Dhar TG, Wu H, Guo W, Cavallaro C, Van Kirk K, Yarde M, Briceno SW, Grafstrom RR, Liu R, Patel SR, Tebben AJ, Camac D, Khan J, Watson A, Yang G, Rose A, Foster WR, Cvijic ME, Davies P, Hynes J Jr. Gardner DS, et al. Among authors: duncia jv. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3833-40. doi: 10.1016/j.bmcl.2013.04.079. Epub 2013 May 7. Bioorg Med Chem Lett. 2013. PMID: 23707259
Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis.
Santella JB 3rd, Gardner DS, Duncia JV, Wu H, Dhar M, Cavallaro C, Tebben AJ, Carter PH, Barrish JC, Yarde M, Briceno SW, Cvijic ME, Grafstrom RR, Liu R, Patel SR, Watson AJ, Yang G, Rose AV, Vickery RD, Caceres-Cortes J, Caporuscio C, Camac DM, Khan JA, An Y, Foster WR, Davies P, Hynes J Jr. Santella JB 3rd, et al. Among authors: duncia jv. J Med Chem. 2014 Sep 25;57(18):7550-64. doi: 10.1021/jm5003167. Epub 2014 Sep 3. J Med Chem. 2014. PMID: 25101488
Beyond U0126. Dianion chemistry leading to the rapid synthesis of a series of potent MEK inhibitors.
Wityak J, Hobbs FW, Gardner DS, Santella JB 3rd, Petraitis JJ, Sun JH, Favata MF, Daulerio AJ, Horiuchi KY, Copeland RA, Scherle PA, Jaffe BD, Trzaskos JM, Magolda RL, Trainor GL, Duncia JV. Wityak J, et al. Among authors: duncia jv. Bioorg Med Chem Lett. 2004 Mar 22;14(6):1483-6. doi: 10.1016/j.bmcl.2004.01.012. Bioorg Med Chem Lett. 2004. PMID: 15006386
Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.
Carter PH, Brown GD, Cherney RJ, Batt DG, Chen J, Clark CM, Cvijic ME, Duncia JV, Ko SS, Mandlekar S, Mo R, Nelson DJ, Pang J, Rose AV, Santella JB 3rd, Tebben AJ, Traeger SC, Xu S, Zhao Q, Barrish JC. Carter PH, et al. Among authors: duncia jv. ACS Med Chem Lett. 2015 Mar 4;6(4):439-44. doi: 10.1021/ml500505q. eCollection 2015 Apr 9. ACS Med Chem Lett. 2015. PMID: 25893046 Free PMC article.
49 results