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Page 1
Discovery of HC-7366: An Orally Bioavailable and Efficacious GCN2 Kinase Activator.
Thomson CG, Aicher TD, Cheng W, Du H, Dudgeon C, Li AH, Li B, Lightcap E, Luo D, Mulvihill M, Pan P, Rahemtulla BF, Rigby AC, Sherborne B, Sood S, Surguladze D, Talbot EPA, Tameire F, Taylor S, Wang Y, Wojnarowicz P, Xiao F, Ramurthy S. Thomson CG, et al. Among authors: aicher td. J Med Chem. 2024 Apr 11;67(7):5259-5271. doi: 10.1021/acs.jmedchem.3c02384. Epub 2024 Mar 26. J Med Chem. 2024. PMID: 38530741
Discovery of LYC-55716: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ) Agonist for Use in Treating Cancer.
Aicher TD, Van Huis CA, Hurd AR, Skalitzky DJ, Taylor CB, Beleh OM, Glick G, Toogood PL, Yang B, Zheng T, Huo C, Gao J, Qiao C, Tian X, Zhang J, Demock K, Hao LY, Lesch CA, Morgan RW, Moisan J, Wang Y, Scatina J, Paulos CM, Zou W, Carter LL, Hu X. Aicher TD, et al. J Med Chem. 2021 Sep 23;64(18):13410-13428. doi: 10.1021/acs.jmedchem.1c00731. Epub 2021 Sep 9. J Med Chem. 2021. PMID: 34499493
Discovery of 2-pyridylureas as glucokinase activators.
Hinklin RJ, Aicher TD, Anderson DA, Baer BR, Boyd SA, Condroski KR, DeWolf WE Jr, Kraser CF, McVean M, Rhodes SP, Sturgis HL, Voegtli WC, Williams L, Houze JB. Hinklin RJ, et al. Among authors: aicher td. J Med Chem. 2014 Oct 9;57(19):8180-6. doi: 10.1021/jm501204z. Epub 2014 Sep 17. J Med Chem. 2014. PMID: 25203462
Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator.
Hinklin RJ, Baer BR, Boyd SA, Chicarelli MD, Condroski KR, DeWolf WE Jr, Fischer J, Frank M, Hingorani GP, Lee PA, Neitzel NA, Pratt SA, Singh A, Sullivan FX, Turner T, Voegtli WC, Wallace EM, Williams L, Aicher TD. Hinklin RJ, et al. Among authors: aicher td. Bioorg Med Chem. 2020 Jan 1;28(1):115232. doi: 10.1016/j.bmc.2019.115232. Epub 2019 Dec 2. Bioorg Med Chem. 2020. PMID: 31818630
C5-Alkyl-2-methylurea-Substituted Pyridines as a New Class of Glucokinase Activators.
Du X, Hinklin RJ, Xiong Y, Dransfield P, Park J, Kohn TJ, Pattaropong V, Lai S, Fu Z, Jiao X, Chow D, Jin L, Davda J, Veniant MM, Anderson DA, Baer BR, Bencsik JR, Boyd SA, Chicarelli MJ, Mohr PJ, Wang B, Condroski KR, DeWolf WE, Conn M, Tran T, Yang J, Aicher TD, Medina JC, Coward P, Houze JB. Du X, et al. Among authors: aicher td. ACS Med Chem Lett. 2014 Nov 22;5(12):1284-9. doi: 10.1021/ml500341w. eCollection 2014 Dec 11. ACS Med Chem Lett. 2014. PMID: 25516785 Free PMC article.
Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394.
Dransfield PJ, Pattaropong V, Lai S, Fu Z, Kohn TJ, Du X, Cheng A, Xiong Y, Komorowski R, Jin L, Conn M, Tien E, DeWolf WE Jr, Hinklin RJ, Aicher TD, Kraser CF, Boyd SA, Voegtli WC, Condroski KR, Veniant-Ellison M, Medina JC, Houze J, Coward P. Dransfield PJ, et al. Among authors: aicher td. ACS Med Chem Lett. 2016 May 23;7(7):714-8. doi: 10.1021/acsmedchemlett.6b00140. eCollection 2016 Jul 14. ACS Med Chem Lett. 2016. PMID: 27437083 Free PMC article.
Secondary amides of (R)-3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase.
Aicher TD, Anderson RC, Gao J, Shetty SS, Coppola GM, Stanton JL, Knorr DC, Sperbeck DM, Brand LJ, Vinluan CC, Kaplan EL, Dragland CJ, Tomaselli HC, Islam A, Lozito RJ, Liu X, Maniara WM, Fillers WS, DelGrande D, Walter RE, Mann WR. Aicher TD, et al. J Med Chem. 2000 Jan 27;43(2):236-49. doi: 10.1021/jm990358+. J Med Chem. 2000. PMID: 10649979
(R)-3,3,3-Trifluoro-2-hydroxy-2-methylpropionamides are orally active inhibitors of pyruvate dehydrogenase kinase.
Aicher TD, Anderson RC, Bebernitz GR, Coppola GM, Jewell CF, Knorr DC, Liu C, Sperbeck DM, Brand LJ, Strohschein RJ, Gao J, Vinluan CC, Shetty SS, Dragland C, Kaplan EL, DelGrande D, Islam A, Liu X, Lozito RJ, Maniara WM, Walter RE, Mann WR. Aicher TD, et al. J Med Chem. 1999 Jul 29;42(15):2741-6. doi: 10.1021/jm9902584. J Med Chem. 1999. PMID: 10425084 No abstract available.
26 results