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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: zhang c. 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 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: zhang c. 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: zhang c. 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 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. 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
Identification of ADAM10 as a major source of HER2 ectodomain sheddase activity in HER2 overexpressing breast cancer cells.
Liu PC, Liu X, Li Y, Covington M, Wynn R, Huber R, Hillman M, Yang G, Ellis D, Marando C, Katiyar K, Bradley J, Abremski K, Stow M, Rupar M, Zhuo J, Li YL, Lin Q, Burns D, Xu M, Zhang C, Qian DQ, He C, Sharief V, Weng L, Agrios C, Shi E, Metcalf B, Newton R, Friedman S, Yao W, Scherle P, Hollis G, Burn TC. Liu PC, et al. Among authors: zhang c. Cancer Biol Ther. 2006 Jun;5(6):657-64. doi: 10.4161/cbt.5.6.2708. Epub 2006 Jun 14. Cancer Biol Ther. 2006. PMID: 16627989 Free article.
Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.
Wu L, Zhang C, He C, Qian D, Lu L, Sun Y, Xu M, Zhuo J, Liu PCC, Klabe R, Wynn R, Covington M, Gallagher K, Leffet L, Bowman K, Diamond S, Koblish H, Zhang Y, Soloviev M, Hollis G, Burn TC, Scherle P, Yeleswaram S, Huber R, Yao W. Wu L, et al. Among authors: zhang c, zhang y. J Med Chem. 2021 Aug 12;64(15):10666-10679. doi: 10.1021/acs.jmedchem.1c00713. Epub 2021 Jul 16. J Med Chem. 2021. PMID: 34269576
Discovery of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK2.
Nguyen MH, Atasoylu O, Wu L, Kapilashrami K, Pusey M, Gallagher K, Lai CT, Zhao P, Barbosa J, Liu K, He C, Zhang C, Styduhar ED, Witten MR, Chen Y, Lin L, Yang YO, Covington M, Diamond S, Yeleswaram S, Yao W. Nguyen MH, et al. Among authors: zhang c. ACS Med Chem Lett. 2022 Jun 22;13(7):1159-1164. doi: 10.1021/acsmedchemlett.2c00206. eCollection 2022 Jul 14. ACS Med Chem Lett. 2022. PMID: 35859885 Free PMC article.
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