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97 results

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Page 1
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: ko ss. 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 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: ko ss. 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.
Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.
Srivastava AS, Ko S, Watterson SH, Pattoli MA, Skala S, Cheng L, Obermeier MT, Vickery R, Discenza LN, D'Arienzo CJ, Gillooly KM, Taylor TL, Pulicicchio C, McIntyre KW, Yip S, Li P, Sun D, Wu DR, Dai J, Wang C, Zhang Y, Wang B, Pawluczyk J, Kempson J, Zhao R, Hou X, Rampulla R, Mathur A, Galella MA, Salter-Cid L, Barrish JC, Carter PH, Fura A, Burke JR, Tino JA. Srivastava AS, et al. ACS Med Chem Lett. 2020 Sep 16;11(11):2195-2203. doi: 10.1021/acsmedchemlett.0c00335. eCollection 2020 Nov 12. ACS Med Chem Lett. 2020. PMID: 33214829 Free PMC article.
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: ko ss. 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
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: ko ss. J Med Chem. 2005 Mar 24;48(6):2194-211. doi: 10.1021/jm049530m. J Med Chem. 2005. PMID: 15771462
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: ko ss. 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: ko ss. 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
Identification of Tricyclic Agonists of Sphingosine-1-phosphate Receptor 1 (S1P1) Employing Ligand-Based Drug Design.
Xiao HY, Watterson SH, Langevine CM, Srivastava AS, Ko SS, Zhang Y, Cherney RJ, Guo WW, Gilmore JL, Sheppeck JE 2nd, Wu DR, Li P, Ramasamy D, Arunachalam P, Mathur A, Taylor TL, Shuster DJ, McIntyre KW, Shen DR, Yarde M, Cvijic ME, Marino AM, Balimane PV, Yang Z, Banas DM, Cornelius G, D'Arienzo CJ, Warrack BM, Lehman-McKeeman L, Salter-Cid LM, Xie J, Barrish JC, Carter PH, Dyckman AJ, Dhar TG. Xiao HY, et al. Among authors: ko ss. J Med Chem. 2016 Nov 10;59(21):9837-9854. doi: 10.1021/acs.jmedchem.6b01099. Epub 2016 Oct 20. J Med Chem. 2016. PMID: 27726358
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: ko ss. 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
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: ko ss. 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
97 results