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342 results

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Page 1
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: metcalf b. 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
Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition.
Burns DM, Li YL, Shi E, He C, Xu M, Zhuo J, Zhang C, Qian DQ, Li Y, Wynn R, Covington MB, Katiyar K, Marando CA, Fridman JS, Scherle P, Friedman S, Metcalf B, Yao W. Burns DM, et al. Among authors: metcalf b. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3525-30. doi: 10.1016/j.bmcl.2009.04.143. Epub 2009 May 5. Bioorg Med Chem Lett. 2009. PMID: 19457660
Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach.
Zhang C, Xu M, He C, Zhuo J, Burns DM, Qian DQ, Lin Q, Li YL, Chen L, Shi E, Agrios C, Weng L, Sharief V, Jalluri R, Li Y, Scherle P, Diamond S, Hunter D, Covington M, Marando C, Wynn R, Katiyar K, Contel N, Vaddi K, Yeleswaram S, Hollis G, Huber R, Friedman S, Metcalf B, Yao W. Zhang C, et al. Among authors: metcalf b. Bioorg Med Chem Lett. 2022 Aug 1;69:128782. doi: 10.1016/j.bmcl.2022.128782. Epub 2022 May 7. Bioorg Med Chem Lett. 2022. PMID: 35537608
Potent benzimidazole sulfonamide protein tyrosine phosphatase 1B inhibitors containing the heterocyclic (S)-isothiazolidinone phosphotyrosine mimetic.
Combs AP, Zhu W, Crawley ML, Glass B, Polam P, Sparks RB, Modi D, Takvorian A, McLaughlin E, Yue EW, Wasserman Z, Bower M, Wei M, Rupar M, Ala PJ, Reid BM, Ellis D, Gonneville L, Emm T, Taylor N, Yeleswaram S, Li Y, Wynn R, Burn TC, Hollis G, Liu PC, Metcalf B. Combs AP, et al. Among authors: metcalf b. J Med Chem. 2006 Jun 29;49(13):3774-89. doi: 10.1021/jm0600904. J Med Chem. 2006. PMID: 16789735
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: metcalf b. J Med Chem. 2007 Feb 22;50(4):603-6. doi: 10.1021/jm061344o. Epub 2007 Jan 26. J Med Chem. 2007. PMID: 17256836
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: metcalf b. 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 potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model.
Yue EW, Douty B, Wayland B, Bower M, Liu X, Leffet L, Wang Q, Bowman KJ, Hansbury MJ, Liu C, Wei M, Li Y, Wynn R, Burn TC, Koblish HK, Fridman JS, Metcalf B, Scherle PA, Combs AP. Yue EW, et al. Among authors: metcalf b. J Med Chem. 2009 Dec 10;52(23):7364-7. doi: 10.1021/jm900518f. J Med Chem. 2009. PMID: 19507862
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: metcalf b. 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
342 results