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Page 1
Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria.
Taft BR, Yokokawa F, Kirrane T, Mata AC, Huang R, Blaquiere N, Waldron G, Zou B, Simon O, Vankadara S, Chan WL, Ding M, Sim S, Straimer J, Guiguemde A, Lakshminarayana SB, Jain JP, Bodenreider C, Thompson C, Lanshoeft C, Shu W, Fang E, Qumber J, Chan K, Pei L, Chen YL, Schulz H, Lim J, Abas SN, Ang X, Liu Y, Angulo-Barturen I, Jiménez-Díaz MB, Gamo FJ, Crespo-Fernandez B, Rosenthal PJ, Cooper RA, Tumwebaze P, Aguiar ACC, Campo B, Campbell S, Wagner J, Diagana TT, Sarko C. Taft BR, et al. Among authors: sarko c. J Med Chem. 2022 Mar 10;65(5):3798-3813. doi: 10.1021/acs.jmedchem.1c01995. Epub 2022 Mar 1. J Med Chem. 2022. PMID: 35229610 Free PMC article.
Indole RSK inhibitors. Part 1: discovery and initial SAR.
Boyer SJ, Burke J, Guo X, Kirrane TM, Snow RJ, Zhang Y, Sarko C, Soleymanzadeh L, Swinamer A, Westbrook J, Dicapua F, Padyana A, Cogan D, Gao A, Xiong Z, Madwed JB, Kashem M, Kugler S, O'Neill MM. Boyer SJ, et al. Among authors: sarko c. Bioorg Med Chem Lett. 2012 Jan 1;22(1):733-7. doi: 10.1016/j.bmcl.2011.10.030. Epub 2011 Oct 14. Bioorg Med Chem Lett. 2012. PMID: 22100312
NITD-688, a pan-serotype inhibitor of the dengue virus NS4B protein, shows favorable pharmacokinetics and efficacy in preclinical animal models.
Moquin SA, Simon O, Karuna R, Lakshminarayana SB, Yokokawa F, Wang F, Saravanan C, Zhang J, Day CW, Chan K, Wang QY, Lu S, Dong H, Wan KF, Lim SP, Liu W, Seh CC, Chen YL, Xu H, Barkan DT, Kounde CS, Sim WLS, Wang G, Yeo HQ, Zou B, Chan WL, Ding M, Song JG, Li M, Osborne C, Blasco F, Sarko C, Beer D, Bonamy GMC, Sasseville VG, Shi PY, Diagana TT, Yeung BKS, Gu F. Moquin SA, et al. Among authors: sarko c. Sci Transl Med. 2021 Feb 3;13(579):eabb2181. doi: 10.1126/scitranslmed.abb2181. Sci Transl Med. 2021. PMID: 33536278
Discovery of Novel Quinoline-Based Proteasome Inhibitors for Human African Trypanosomiasis (HAT).
Koester DC, Marx VM, Williams S, Jiricek J, Dauphinais M, René O, Miller SL, Zhang L, Patra D, Chen YL, Cheung H, Gable J, Lakshminarayana SB, Osborne C, Galarneau JR, Kulkarni U, Richmond W, Bretz A, Xiao L, Supek F, Wiesmann C, Honnappa S, Be C, Mäser P, Kaiser M, Ritchie R, Barrett MP, Diagana TT, Sarko C, Rao SPS. Koester DC, et al. Among authors: sarko c. J Med Chem. 2022 Sep 8;65(17):11776-11787. doi: 10.1021/acs.jmedchem.2c00791. Epub 2022 Aug 22. J Med Chem. 2022. PMID: 35993839 Free PMC article.
Cyanotriazoles are selective topoisomerase II poisons that rapidly cure trypanosome infections.
Rao SPS, Gould MK, Noeske J, Saldivia M, Jumani RS, Ng PS, René O, Chen YL, Kaiser M, Ritchie R, Francisco AF, Johnson N, Patra D, Cheung H, Deniston C, Schenk AD, Cortopassi WA, Schmidt RS, Wiedemar N, Thomas B, Palkar R, Ghafar NA, Manoharan V, Luu C, Gable JE, Wan KF, Myburgh E, Mottram JC, Barnes W, Walker J, Wartchow C, Aziz N, Osborne C, Wagner J, Sarko C, Kelly JM, Manjunatha UH, Mäser P, Jiricek J, Lakshminarayana SB, Barrett MP, Diagana TT. Rao SPS, et al. Among authors: sarko c. Science. 2023 Jun 30;380(6652):1349-1356. doi: 10.1126/science.adh0614. Epub 2023 Jun 29. Science. 2023. PMID: 37384702 Free article.
Evolution of the thienopyridine class of inhibitors of IkappaB kinase-beta: part I: hit-to-lead strategies.
Morwick T, Berry A, Brickwood J, Cardozo M, Catron K, DeTuri M, Emeigh J, Homon C, Hrapchak M, Jacober S, Jakes S, Kaplita P, Kelly TA, Ksiazek J, Liuzzi M, Magolda R, Mao C, Marshall D, McNeil D, Prokopowicz A 3rd, Sarko C, Scouten E, Sledziona C, Sun S, Watrous J, Wu JP, Cywin CL. Morwick T, et al. Among authors: sarko c. J Med Chem. 2006 May 18;49(10):2898-908. doi: 10.1021/jm0510979. J Med Chem. 2006. PMID: 16686533
Discovery and design of benzimidazolone based inhibitors of p38 MAP kinase.
Hammach A, Barbosa A, Gaenzler FC, Fadra T, Goldberg D, Hao MH, Kroe RR, Liu P, Qian KC, Ralph M, Sarko C, Soleymanzadeh F, Moss N. Hammach A, et al. Among authors: sarko c. Bioorg Med Chem Lett. 2006 Dec 15;16(24):6316-20. doi: 10.1016/j.bmcl.2006.09.014. Epub 2006 Sep 28. Bioorg Med Chem Lett. 2006. PMID: 17010605
Discovery and optimization of pyrazole amides as antagonists of CCR1.
Harcken C, Sarko C, Mao C, Lord J, Raudenbush B, Razavi H, Liu P, Swinamer A, Disalvo D, Lee T, Lin S, Kukulka A, Grbic H, Patel M, Patel M, Fletcher K, Joseph D, White D, Amodeo L, Berg K, Brown M, Thomson DS. Harcken C, et al. Among authors: sarko c. Bioorg Med Chem Lett. 2019 Feb 1;29(3):435-440. doi: 10.1016/j.bmcl.2018.11.015. Epub 2018 Nov 9. Bioorg Med Chem Lett. 2019. PMID: 30455146
A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties.
Moss N, Choi Y, Cogan D, Flegg A, Kahrs A, Loke P, Meyn O, Nagaraja R, Napier S, Parker A, Thomas Peterson J, Ramsden P, Sarko C, Skow D, Tomlinson J, Tye H, Whitaker M. Moss N, et al. Among authors: sarko c. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2206-10. doi: 10.1016/j.bmcl.2009.02.126. Epub 2009 Mar 9. Bioorg Med Chem Lett. 2009. PMID: 19307114
19 results