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177 results

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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: gardner ds. 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: gardner ds. 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
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: gardner ds. 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 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: gardner ds. 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: gardner ds. 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. 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
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. 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: gardner ds. J Med Chem. 2014 Sep 25;57(18):7550-64. doi: 10.1021/jm5003167. Epub 2014 Sep 3. J Med Chem. 2014. PMID: 25101488
Use of a Conformational-Switching Mechanism to Modulate Exposed Polarity: Discovery of CCR2 Antagonist BMS-741672.
Yang MG, Xiao Z, Cherney RJ, Tebben AJ, Batt DG, Brown GD, Chen J, Cvijic ME, Dabros M, Duncia JV, Galella M, Gardner DS, Khandelwal P, Ko SS, Malley MF, Mo R, Pang J, Rose AV, Santella JB 3rd, Shi H, Srivastava A, Traeger SC, Wang B, Xu S, Zhao R, Barrish JC, Mandlekar S, Zhao Q, Carter PH. Yang MG, et al. Among authors: gardner ds. ACS Med Chem Lett. 2019 Jan 16;10(3):300-305. doi: 10.1021/acsmedchemlett.8b00439. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891130 Free PMC article.
Discovery of BMS-753426: A Potent Orally Bioavailable Antagonist of CC Chemokine Receptor 2.
Yang MG, Xiao Z, Zhao R, Tebben AJ, Wang B, Cherney RJ, Batt DG, Brown GD, Cvijic ME, Duncia JV, Gallela MA, Gardner DS, Khandelwal P, Malley MF, Pang J, Rose AV, Santella JB 3rd, Sarjeant AA, Xu S, Mathur A, Mandlekar S, Vuppugalla R, Zhao Q, Carter PH. Yang MG, et al. Among authors: gardner ds. ACS Med Chem Lett. 2021 May 25;12(6):969-975. doi: 10.1021/acsmedchemlett.1c00082. eCollection 2021 Jun 10. ACS Med Chem Lett. 2021. PMID: 34141082 Free PMC article.
177 results