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78 results

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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: yeleswaram s. 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
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: yeleswaram s. J Med Chem. 2005 Mar 24;48(6):2194-211. doi: 10.1021/jm049530m. J Med Chem. 2005. PMID: 15771462
Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.
Yao W, Zhuo J, Burns DM, Xu M, Zhang C, Li YL, Qian DQ, He C, Weng L, Shi E, Lin Q, Agrios C, Burn TC, Caulder E, Covington MB, Fridman JS, Friedman S, Katiyar K, Hollis G, Li Y, Liu C, Liu X, Marando CA, Newton R, Pan M, Scherle P, Taylor N, Vaddi K, Wasserman ZR, Wynn R, Yeleswaram S, Jalluri R, Bower M, Zhou BB, Metcalf B. Yao W, et al. Among authors: yeleswaram s. J Med Chem. 2007 Feb 22;50(4):603-6. doi: 10.1021/jm061344o. Epub 2007 Jan 26. J Med Chem. 2007. PMID: 17256836
3-[(5-Chloro-2-hydroxyphenyl)methyl]-5-[4-(trifluoromethyl)phenyl ]-1,3,4-oxadiazol-2(3H)-one, BMS-191011: opener of large-conductance Ca(2+)-activated potassium (maxi-K) channels, identification, solubility, and SAR.
Romine JL, Martin SW, Meanwell NA, Gribkoff VK, Boissard CG, Dworetzky SI, Natale J, Moon S, Ortiz A, Yeleswaram S, Pajor L, Gao Q, Starrett JE Jr. Romine JL, et al. Among authors: yeleswaram s. J Med Chem. 2007 Feb 8;50(3):528-42. doi: 10.1021/jm061006n. J Med Chem. 2007. PMID: 17266205
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: yeleswaram s. 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
Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations.
Burns DM, He C, Li Y, Scherle P, Liu X, Marando CA, Covington MB, Yang G, Pan M, Turner S, Fridman JS, Hollis G, Vaddi K, Yeleswaram S, Newton R, Friedman S, Metcalf B, Yao W. Burns DM, et al. Among authors: yeleswaram s. Bioorg Med Chem Lett. 2008 Jan 15;18(2):560-4. doi: 10.1016/j.bmcl.2007.11.086. Epub 2007 Nov 28. Bioorg Med Chem Lett. 2008. PMID: 18068976
Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.
Yao W, Zhuo J, Burns DM, Li YL, Qian DQ, Zhang C, He C, Xu M, Shi E, Li Y, Marando CA, Covington MB, Yang G, Liu X, Pan M, Fridman JS, Scherle P, Wasserman ZR, Hollis G, Vaddi K, Yeleswaram S, Newton R, Friedman S, Metcalf B. Yao W, et al. Among authors: yeleswaram s. Bioorg Med Chem Lett. 2008 Jan 1;18(1):159-63. doi: 10.1016/j.bmcl.2007.10.108. Epub 2007 Nov 4. Bioorg Med Chem Lett. 2008. PMID: 18036818
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
Xue CB, Wang A, Meloni D, Zhang K, Kong L, Feng H, Glenn J, Huang T, Zhang Y, Cao G, Anand R, Zheng C, Xia M, Han Q, Robinson DJ, Storace L, Shao L, Li M, Brodmerkel CM, Covington M, Scherle P, Diamond S, Yeleswaram S, Vaddi K, Newton R, Hollis G, Friedman S, Metcalf B. Xue CB, et al. Among authors: yeleswaram s. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7473-8. doi: 10.1016/j.bmcl.2010.10.020. Epub 2010 Oct 13. Bioorg Med Chem Lett. 2010. PMID: 21036044
78 results