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Page 1
Paradoxical Increase of Permeability and Lipophilicity with the Increasing Topological Polar Surface Area within a Series of PRMT5 Inhibitors.
Argikar U, Blatter M, Bednarczyk D, Chen Z, Cho YS, Doré M, Dumouchel JL, Ho S, Hoegenauer K, Kawanami T, Mathieu S, Meredith E, Möbitz H, Murphy SK, Parthasarathy S, Soldermann CP, Santos J, Silver S, Skolnik S, Stojanovic A. Argikar U, et al. Among authors: meredith e. J Med Chem. 2022 Sep 22;65(18):12386-12402. doi: 10.1021/acs.jmedchem.2c01068. Epub 2022 Sep 7. J Med Chem. 2022. PMID: 36069672
Structure based design of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors from a phenotypic screen.
Palacios DS, Meredith E, Kawanami T, Adams C, Chen X, Darsigny V, Geno E, Palermo M, Baird D, Boynton G, Busby SA, George EL, Guy C, Hewett J, Tierney L, Thigale S, Weihofen W, Wang L, White N, Yin M, Argikar UA. Palacios DS, et al. Among authors: meredith e. Bioorg Med Chem Lett. 2018 Feb 1;28(3):365-370. doi: 10.1016/j.bmcl.2017.12.037. Epub 2017 Dec 18. Bioorg Med Chem Lett. 2018. PMID: 29275937
Scaffold Morphing Identifies 3-Pyridyl Azetidine Ureas as Inhibitors of Nicotinamide Phosphoribosyltransferase (NAMPT).
Palacios DS, Meredith EL, Kawanami T, Adams CM, Chen X, Darsigny V, Palermo M, Baird D, George EL, Guy C, Hewett J, Tierney L, Thigale S, Wang L, Weihofen WA. Palacios DS, et al. ACS Med Chem Lett. 2019 Oct 10;10(11):1524-1529. doi: 10.1021/acsmedchemlett.9b00325. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749905 Free PMC article.
Identification of orally available naphthyridine protein kinase D inhibitors.
Meredith EL, Ardayfio O, Beattie K, Dobler MR, Enyedy I, Gaul C, Hosagrahara V, Jewell C, Koch K, Lee W, Lehmann H, McKinsey TA, Miranda K, Pagratis N, Pancost M, Patnaik A, Phan D, Plato C, Qian M, Rajaraman V, Rao C, Rozhitskaya O, Ruppen T, Shi J, Siska SJ, Springer C, van Eis M, Vega RB, von Matt A, Yang L, Yoon T, Zhang JH, Zhu N, Monovich LG. Meredith EL, et al. J Med Chem. 2010 Aug 12;53(15):5400-21. doi: 10.1021/jm100075z. J Med Chem. 2010. PMID: 20684591
Identification of potent and selective amidobipyridyl inhibitors of protein kinase D.
Meredith EL, Beattie K, Burgis R, Capparelli M, Chapo J, Dipietro L, Gamber G, Enyedy I, Hood DB, Hosagrahara V, Jewell C, Koch KA, Lee W, Lemon DD, McKinsey TA, Miranda K, Pagratis N, Phan D, Plato C, Rao C, Rozhitskaya O, Soldermann N, Springer C, van Eis M, Vega RB, Yan W, Zhu Q, Monovich LG. Meredith EL, et al. J Med Chem. 2010 Aug 12;53(15):5422-38. doi: 10.1021/jm100076w. J Med Chem. 2010. PMID: 20684592
The Discovery of ( S)-1-(6-(3-((4-(1-(Cyclopropanecarbonyl)piperidin-4-yl)-2-methylphenyl)amino)-2,3-dihydro-1 H-inden-4-yl)pyridin-2-yl)-5-methyl-1 H-pyrazole-4-carboxylic Acid, a Soluble Guanylate Cyclase Activator Specifically Designed for Topical Ocular Delivery as a Therapy for Glaucoma.
Ehara T, Adams CM, Bevan D, Ji N, Meredith EL, Belanger DB, Powers J, Kato M, Solovay C, Liu D, Capparelli M, Bolduc P, Grob JE, Daniels MH, Ferrara L, Yang L, Li B, Towler CS, Stacy RC, Prasanna G, Mogi M. Ehara T, et al. Among authors: meredith el. J Med Chem. 2018 Mar 22;61(6):2552-2570. doi: 10.1021/acs.jmedchem.8b00007. Epub 2018 Mar 2. J Med Chem. 2018. PMID: 29498522
Discovery of Oral VEGFR-2 Inhibitors with Prolonged Ocular Retention That Are Efficacious in Models of Wet Age-Related Macular Degeneration.
Meredith EL, Mainolfi N, Poor S, Qiu Y, Miranda K, Powers J, Liu D, Ma F, Solovay C, Rao C, Johnson L, Ji N, Artman G, Hardegger L, Hanks S, Shen S, Woolfenden A, Fassbender E, Sivak JM, Zhang Y, Long D, Cepeda R, Liu F, Hosagrahara VP, Lee W, Tarsa P, Anderson K, Elliott J, Jaffee B. Meredith EL, et al. J Med Chem. 2015 Dec 10;58(23):9273-86. doi: 10.1021/acs.jmedchem.5b01227. Epub 2015 Nov 30. J Med Chem. 2015. PMID: 26568411
The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration.
Adams CM, Anderson K, Artman G 3rd, Bizec JC, Cepeda R, Elliott J, Fassbender E, Ghosh M, Hanks S, Hardegger LA, Hosagrahara VP, Jaffee B, Jendza K, Ji N, Johnson L, Lee W, Liu D, Liu F, Long D, Ma F, Mainolfi N, Meredith EL, Miranda K, Peng Y, Poor S, Powers J, Qiu Y, Rao C, Shen S, Sivak JM, Solovay C, Tarsa P, Woolfenden A, Zhang C, Zhang Y. Adams CM, et al. Among authors: meredith el. J Med Chem. 2018 Feb 22;61(4):1622-1635. doi: 10.1021/acs.jmedchem.7b01731. Epub 2018 Feb 5. J Med Chem. 2018. PMID: 29400470
Nicotinamide Phosphoribosyltransferase Inhibitor as a Novel Payload for Antibody-Drug Conjugates.
Karpov AS, Abrams T, Clark S, Raikar A, D'Alessio JA, Dillon MP, Gesner TG, Jones D, Lacaud M, Mallet W, Martyniuk P, Meredith E, Mohseni M, Nieto-Oberhuber CM, Palacios D, Perruccio F, Piizzi G, Zurini M, Bialucha CU. Karpov AS, et al. Among authors: meredith e. ACS Med Chem Lett. 2018 Jun 28;9(8):838-842. doi: 10.1021/acsmedchemlett.8b00254. eCollection 2018 Aug 9. ACS Med Chem Lett. 2018. PMID: 30128077 Free PMC article.
79 results