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Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces parasite growth in vitro.
Preuss J, Maloney P, Peddibhotla S, Hedrick MP, Hershberger P, Gosalia P, Milewski M, Li YL, Sugarman E, Hood B, Suyama E, Nguyen K, Vasile S, Sergienko E, Mangravita-Novo A, Vicchiarelli M, McAnally D, Smith LH, Roth GP, Diwan J, Chung TD, Jortzik E, Rahlfs S, Becker K, Pinkerton AB, Bode L. Preuss J, et al. Among authors: smith lh. J Med Chem. 2012 Aug 23;55(16):7262-72. doi: 10.1021/jm300833h. Epub 2012 Aug 6. J Med Chem. 2012. PMID: 22813531 Free PMC article.
Imidazole-derived agonists for the neurotensin 1 receptor.
Hershberger PM, Hedrick MP, Peddibhotla S, Mangravita-Novo A, Gosalia P, Li Y, Gray W, Vicchiarelli M, Smith LH, Chung TD, Thomas JB, Caron MG, Pinkerton AB, Barak LS, Roth GP. Hershberger PM, et al. Among authors: smith lh. Bioorg Med Chem Lett. 2014 Jan 1;24(1):262-7. doi: 10.1016/j.bmcl.2013.11.026. Epub 2013 Nov 21. Bioorg Med Chem Lett. 2014. PMID: 24332089 Free PMC article.
Discovery of ML314, a Brain Penetrant Non-Peptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.
Peddibhotla S, Hedrick MP, Hershberger P, Maloney PR, Li Y, Milewski M, Gosalia P, Gray W, Mehta A, Sugarman E, Hood B, Suyama E, Nguyen K, Heynen-Genel S, Vasile S, Salaniwal S, Stonich D, Su Y, Mangravita-Novo A, Vicchiarelli M, Roth GP, Smith LH, Chung TD, Hanson GR, Thomas JB, Caron MG, Barak LS, Pinkerton AB. Peddibhotla S, et al. Among authors: smith lh. ACS Med Chem Lett. 2013 Jul 20;4(9):846-851. doi: 10.1021/ml400176n. ACS Med Chem Lett. 2013. PMID: 24611085 Free PMC article.
Discovery of Sulfonamidebenzamides as Selective Apoptotic CHOP Pathway Activators of the Unfolded Protein Response.
Flaherty DP, Miller JR, Garshott DM, Hedrick M, Gosalia P, Li Y, Milewski M, Sugarman E, Vasile S, Salaniwal S, Su Y, Smith LH, Chung TD, Pinkerton AB, Aubé J, Callaghan MU, Golden JE, Fribley AM, Kaufman RJ. Flaherty DP, et al. Among authors: smith lh. ACS Med Chem Lett. 2014 Oct 29;5(12):1278-1283. doi: 10.1021/ml5003234. eCollection 2014 Dec 11. ACS Med Chem Lett. 2014. PMID: 25530830 Free PMC article.
Discovery of ML358, a Selective Small Molecule Inhibitor of the SKN-1 Pathway Involved in Drug Detoxification and Resistance in Nematodes.
Peddibhotla S, Fontaine P, Leung CK, Maloney P, Hershberger PM, Wang Y, Bousquet MS, Luesch H, Mangravita-Novo A, Pinkerton AB, Smith LH, Malany S, Choe K. Peddibhotla S, et al. Among authors: smith lh. ACS Chem Biol. 2015 Aug 21;10(8):1871-9. doi: 10.1021/acschembio.5b00304. Epub 2015 May 22. ACS Chem Biol. 2015. PMID: 25946346
Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators.
Pinkerton AB, Peddibhotla S, Yamamoto F, Slosky LM, Bai Y, Maloney P, Hershberger P, Hedrick MP, Falter B, Ardecky RJ, Smith LH, Chung TDY, Jackson MR, Caron MG, Barak LS. Pinkerton AB, et al. Among authors: smith lh. J Med Chem. 2019 Sep 12;62(17):8357-8363. doi: 10.1021/acs.jmedchem.9b00340. Epub 2019 Aug 20. J Med Chem. 2019. PMID: 31390201 Free PMC article.
Discovery of small molecule antagonists of chemokine receptor CXCR6 that arrest tumor growth in SK-HEP-1 mouse xenografts as a model of hepatocellular carcinoma.
Peddibhotla S, Hershberger PM, Jason Kirby R, Sugarman E, Maloney PR, Hampton Sessions E, Divlianska D, Morfa CJ, Terry D, Pinkerton AB, Smith LH, Malany S. Peddibhotla S, et al. Among authors: smith lh. Bioorg Med Chem Lett. 2020 Feb 15;30(4):126899. doi: 10.1016/j.bmcl.2019.126899. Epub 2019 Dec 17. Bioorg Med Chem Lett. 2020. PMID: 31882297 Free PMC article.
Optimization of a urea-containing series of nicotinamide phosphoribosyltransferase (NAMPT) activators.
Pinkerton AB, Sessions EH, Hershberger P, Maloney PR, Peddibhotla S, Hopf M, Sergienko E, Ma CT, Smith LH, Jackson MR, Tanaka J, Tsuji T, Akiu M, Cohen SE, Nakamura T, Gardell SJ. Pinkerton AB, et al. Among authors: smith lh. Bioorg Med Chem Lett. 2021 Jun 1;41:128007. doi: 10.1016/j.bmcl.2021.128007. Epub 2021 Mar 31. Bioorg Med Chem Lett. 2021. PMID: 33798699
Inhibition of protein kinase C-driven nuclear factor-kappaB activation: synthesis, structure-activity relationship, and pharmacological profiling of pathway specific benzimidazole probe molecules.
Peddibhotla S, Shi R, Khan P, Smith LH, Mangravita-Novo A, Vicchiarelli M, Su Y, Okolotowicz KJ, Cashman JR, Reed JC, Roth GP. Peddibhotla S, et al. Among authors: smith lh. J Med Chem. 2010 Jun 24;53(12):4793-7. doi: 10.1021/jm1000248. J Med Chem. 2010. PMID: 20481485 Free PMC article.
Potent, selective, and orally available benzoisothiazolone phosphomannose isomerase inhibitors as probes for congenital disorder of glycosylation Ia.
Dahl R, Bravo Y, Sharma V, Ichikawa M, Dhanya RP, Hedrick M, Brown B, Rascon J, Vicchiarelli M, Mangravita-Novo A, Yang L, Stonich D, Su Y, Smith LH, Sergienko E, Freeze HH, Cosford ND. Dahl R, et al. Among authors: smith lh. J Med Chem. 2011 May 26;54(10):3661-8. doi: 10.1021/jm101401a. Epub 2011 May 3. J Med Chem. 2011. PMID: 21539312 Free PMC article.
542 results