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Page 1
Discovery of KIN-3248, An Irreversible, Next Generation FGFR Inhibitor for the Treatment of Advanced Tumors Harboring FGFR2 and/or FGFR3 Gene Alterations.
Tyhonas JS, Arnold LD, Cox JM, Franovic A, Gardiner E, Grandinetti K, Kania R, Kanouni T, Lardy M, Li C, Martin ES, Miller N, Mohan A, Murphy EA, Perez M, Soroceanu L, Timple N, Uryu S, Womble S, Kaldor SW. Tyhonas JS, et al. J Med Chem. 2024 Feb 8;67(3):1734-1746. doi: 10.1021/acs.jmedchem.3c01819. Epub 2024 Jan 24. J Med Chem. 2024. PMID: 38267212
The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition.
Chen YK, Kanouni T, Arnold LD, Cox JM, Gardiner E, Grandinetti K, Jiang P, Kaldor SW, Lee C, Li C, Martin ES, Miller N, Murphy EA, Timple N, Tyhonas JS, Vassar A, Wang TS, Williams R, Yuan D, Kania RS. Chen YK, et al. Among authors: tyhonas js. J Med Chem. 2024 Feb 8;67(3):1747-1757. doi: 10.1021/acs.jmedchem.3c01830. Epub 2024 Jan 17. J Med Chem. 2024. PMID: 38230963
The discovery of (1R, 3R)-1-(3-chloro-5-fluorophenyl)-3-(hydroxymethyl)-1,2,3,4-tetrahydroisoquinoline-6-carbonitrile, a potent and selective agonist of human transient receptor potential cation channel subfamily m member 5 (TRPM5) and evaluation of as a potential gastrointestinal prokinetic agent.
Sabat M, Raveglia LF, Aldegheri L, Barilli A, Bianchi F, Brault L, Brodbeck D, Feriani A, Lingard I, Miura J, Myers R, Piccoli L, Tassini S, Tyhonas J, Ton-Nu T, Wang H, Virginio C. Sabat M, et al. Bioorg Med Chem. 2022 Dec 15;76:117084. doi: 10.1016/j.bmc.2022.117084. Epub 2022 Nov 6. Bioorg Med Chem. 2022. PMID: 36402081
Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure.
Lanier M, Pickens J, Bigi SV, Bradshaw-Pierce EL, Chambers A, Cheruvallath ZS, Cole D, Dougan DR, Ermolieff J, Gibson T, Halkowycz P, Hirokawa A, Ivetac A, Miura J, Nunez E, Sabat M, Tyhonas J, Wang H, Wang X, Swann S. Lanier M, et al. ACS Med Chem Lett. 2017 Feb 8;8(3):316-320. doi: 10.1021/acsmedchemlett.6b00481. eCollection 2017 Mar 9. ACS Med Chem Lett. 2017. PMID: 28337323 Free PMC article.
Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.
Michellys PY, Ardecky RJ, Chen JH, D'Arrigo J, Grese TA, Karanewsky DS, Leibowitz MD, Liu S, Mais DA, Mapes CM, Montrose-Rafizadeh C, Ogilvie KM, Reifel-Miller A, Rungta D, Thompson AW, Tyhonas JS, Boehm MF. Michellys PY, et al. Among authors: tyhonas js. J Med Chem. 2003 Sep 11;46(19):4087-103. doi: 10.1021/jm020401k. J Med Chem. 2003. PMID: 12954061
Novel (2E,4E,6Z)-7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta-2,4,6-trienoic acid retinoid X receptor modulators are active in models of type 2 diabetes.
Michellys PY, Ardecky RJ, Chen JH, Crombie DL, Etgen GJ, Faul MM, Faulkner AL, Grese TA, Heyman RA, Karanewsky DS, Klausing K, Leibowitz MD, Liu S, Mais DA, Mapes CM, Marschke KB, Reifel-Miller A, Ogilvie KM, Rungta D, Thompson AW, Tyhonas JS, Boehm MF. Michellys PY, et al. Among authors: tyhonas js. J Med Chem. 2003 Jun 19;46(13):2683-96. doi: 10.1021/jm020340q. J Med Chem. 2003. PMID: 12801232
5(Z)-benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes as non-steroidal glucocorticoid receptor modulators.
Ardecky RJ, Hudson AR, Phillips DP, Tyhonas JS, Deckhut C, Lau TL, Li Y, Martinborough EA, Roach SL, Higuchi RI, Lopez FJ, Marschke KB, Miner JN, Karanewsky DS, Negro-Vilar A, Zhi L. Ardecky RJ, et al. Among authors: tyhonas js. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4158-62. doi: 10.1016/j.bmcl.2007.05.062. Epub 2007 May 23. Bioorg Med Chem Lett. 2007. PMID: 17553679
Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.
Michellys PY, Boehm MF, Chen JH, Grese TA, Karanewsky DS, Leibowitz MD, Liu S, Mais DA, Mapes CM, Reifel-Miller A, Ogilvie KM, Rungta D, Thompson AW, Tyhonas JS, Yumibe N, Ardecky RJ. Michellys PY, et al. Among authors: tyhonas js. Bioorg Med Chem Lett. 2003 Nov 17;13(22):4071-5. doi: 10.1016/j.bmcl.2003.08.048. Bioorg Med Chem Lett. 2003. PMID: 14592510
Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.
Brooks DA, Etgen GJ, Rito CJ, Shuker AJ, Dominianni SJ, Warshawsky AM, Ardecky R, Paterniti JR, Tyhonas J, Karanewsky DS, Kauffman RF, Broderick CL, Oldham BA, Montrose-Rafizadeh C, Winneroski LL, Faul MM, McCarthy JR. Brooks DA, et al. J Med Chem. 2001 Jun 21;44(13):2061-4. doi: 10.1021/jm0155188. J Med Chem. 2001. PMID: 11405642
Correction to "Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure".
Lanier M, Pickens J, Bigi SV, Bradshaw-Pierce EL, Chambers A, Cheruvallath ZS, Cole D, Dougan DR, Ermolieff J, Gibson T, Halkowycz P, Hirokawa A, Ivetac A, McBride C, Miura J, Nunez E, Sabat M, Tyhonas J, Wang H, Wang X, Swann S. Lanier M, et al. ACS Med Chem Lett. 2017 Nov 8;8(12):1341. doi: 10.1021/acsmedchemlett.7b00457. eCollection 2017 Dec 14. ACS Med Chem Lett. 2017. PMID: 29259759 Free PMC article.
13 results