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Discovery of N-(6-Fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-[(3R)-3-hydroxypyrrolidin-1-yl]thiophene-2-sulfonamide (LSN 3213128), a Potent and Selective Nonclassical Antifolate Aminoimidazole-4-carboxamide Ribonucleotide Formyltransferase (AICARFT) Inhibitor Effective at Tumor Suppression in a Cancer Xenograft Model.
Fales KR, Njoroge FG, Brooks HB, Thibodeaux S, Torrado A, Si C, Toth JL, Mc Cowan JR, Roth KD, Thrasher KJ, Frimpong K, Lee MR, Dally RD, Shepherd TA, Durham TB, Margolis BJ, Wu Z, Wang Y, Atwell S, Wang J, Hui YH, Meier TI, Konicek SA, Geeganage S. Fales KR, et al. Among authors: torrado a. J Med Chem. 2017 Dec 14;60(23):9599-9616. doi: 10.1021/acs.jmedchem.7b01046. Epub 2017 Nov 9. J Med Chem. 2017. PMID: 29072452
Characterization of a novel AICARFT inhibitor which potently elevates ZMP and has anti-tumor activity in murine models.
Brooks HB, Meier TI, Geeganage S, Fales KR, Thrasher KJ, Konicek SA, Spencer CD, Thibodeaux S, Foreman RT, Hui YH, Roth KD, Qian YW, Wang T, Luo S, Torrado A, Si C, Toth JL, Mc Cowan JR, Frimpong K, Lee MR, Dally RD, Shepherd TA, Durham TB, Wang Y, Wu Z, Iversen PW, Njoroge FG. Brooks HB, et al. Among authors: torrado a. Sci Rep. 2018 Oct 18;8(1):15458. doi: 10.1038/s41598-018-33453-4. Sci Rep. 2018. PMID: 30337562 Free PMC article.
Discovery of a novel series of orally active nociceptin/orphanin FQ (NOP) receptor antagonists based on a dihydrospiro(piperidine-4,7'-thieno[2,3-c]pyran) scaffold.
Toledo MA, Pedregal C, Lafuente C, Diaz N, Martinez-Grau MA, Jiménez A, Benito A, Torrado A, Mateos C, Joshi EM, Kahl SD, Rash KS, Mudra DR, Barth VN, Shaw DB, McKinzie D, Witkin JM, Statnick MA. Toledo MA, et al. Among authors: torrado a. J Med Chem. 2014 Apr 24;57(8):3418-29. doi: 10.1021/jm500117r. Epub 2014 Apr 11. J Med Chem. 2014. PMID: 24678969
93 results