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Discovery of IACS-9779 and IACS-70465 as Potent Inhibitors Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme.
Hamilton MM, Mseeh F, McAfoos TJ, Leonard PG, Reyna NJ, Harris AL, Xu A, Han M, Soth MJ, Czako B, Theroff JP, Mandal PK, Burke JP, Virgin-Downey B, Petrocchi A, Pfaffinger D, Rogers NE, Parker CA, Yu SS, Jiang Y, Krapp S, Lammens A, Trevitt G, Tremblay MR, Mikule K, Wilcoxen K, Cross JB, Jones P, Marszalek JR, Lewis RT. Hamilton MM, et al. Among authors: tremblay mr. J Med Chem. 2021 Aug 12;64(15):11302-11329. doi: 10.1021/acs.jmedchem.1c00679. Epub 2021 Jul 22. J Med Chem. 2021. PMID: 34292726
Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R.
Czako B, Marszalek JR, Burke JP, Mandal P, Leonard PG, Cross JB, Mseeh F, Jiang Y, Chang EQ, Suzuki E, Kovacs JJ, Feng N, Gera S, Harris AL, Liu Z, Mullinax RA, Pang J, Parker CA, Spencer ND, Yu SS, Wu Q, Tremblay MR, Mikule K, Wilcoxen K, Heffernan TP, Draetta GF, Jones P. Czako B, et al. Among authors: tremblay mr. J Med Chem. 2020 Sep 10;63(17):9888-9911. doi: 10.1021/acs.jmedchem.0c00936. Epub 2020 Aug 18. J Med Chem. 2020. PMID: 32787110
Synthetic silvestrol analogues as potent and selective protein synthesis inhibitors.
Liu T, Nair SJ, Lescarbeau A, Belani J, Peluso S, Conley J, Tillotson B, O'Hearn P, Smith S, Slocum K, West K, Helble J, Douglas M, Bahadoor A, Ali J, McGovern K, Fritz C, Palombella VJ, Wylie A, Castro AC, Tremblay MR. Liu T, et al. Among authors: tremblay mr. J Med Chem. 2012 Oct 25;55(20):8859-78. doi: 10.1021/jm3011542. Epub 2012 Oct 12. J Med Chem. 2012. PMID: 23025805
Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate.
Evans CA, Liu T, Lescarbeau A, Nair SJ, Grenier L, Pradeilles JA, Glenadel Q, Tibbitts T, Rowley AM, DiNitto JP, Brophy EE, O'Hearn EL, Ali JA, Winkler DG, Goldstein SI, O'Hearn P, Martin CM, Hoyt JG, Soglia JR, Cheung C, Pink MM, Proctor JL, Palombella VJ, Tremblay MR, Castro AC. Evans CA, et al. Among authors: tremblay mr. ACS Med Chem Lett. 2016 Jul 22;7(9):862-7. doi: 10.1021/acsmedchemlett.6b00238. eCollection 2016 Sep 8. ACS Med Chem Lett. 2016. PMID: 27660692 Free PMC article.
Semisynthetic cyclopamine analogues as potent and orally bioavailable hedgehog pathway antagonists.
Tremblay MR, Nevalainen M, Nair SJ, Porter JR, Castro AC, Behnke ML, Yu LC, Hagel M, White K, Faia K, Grenier L, Campbell MJ, Cushing J, Woodward CN, Hoyt J, Foley MA, Read MA, Sydor JR, Tong JK, Palombella VJ, McGovern K, Adams J. Tremblay MR, et al. J Med Chem. 2008 Nov 13;51(21):6646-9. doi: 10.1021/jm8008508. Epub 2008 Oct 9. J Med Chem. 2008. PMID: 18842035
Discovery of a potent and orally active hedgehog pathway antagonist (IPI-926).
Tremblay MR, Lescarbeau A, Grogan MJ, Tan E, Lin G, Austad BC, Yu LC, Behnke ML, Nair SJ, Hagel M, White K, Conley J, Manna JD, Alvarez-Diez TM, Hoyt J, Woodward CN, Sydor JR, Pink M, MacDougall J, Campbell MJ, Cushing J, Ferguson J, Curtis MS, McGovern K, Read MA, Palombella VJ, Adams J, Castro AC. Tremblay MR, et al. J Med Chem. 2009 Jul 23;52(14):4400-18. doi: 10.1021/jm900305z. J Med Chem. 2009. PMID: 19522463
Synthesis and biological evaluation of (-)-laulimalide analogues.
Gallagher BM Jr, Fang FG, Johannes CW, Pesant M, Tremblay MR, Zhao H, Akasaka K, Li XY, Liu J, Littlefield BA. Gallagher BM Jr, et al. Among authors: tremblay mr. Bioorg Med Chem Lett. 2004 Feb 9;14(3):575-9. doi: 10.1016/j.bmcl.2003.12.001. Bioorg Med Chem Lett. 2004. PMID: 14741246
29 results