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Page 1
3,5-Disubstituted-indole-7-carboxamides as IKKβ Inhibitors: Optimization of Oral Activity via the C3 Substituent.
Kerns JK, Busch-Petersen J, Fu W, Boehm JC, Nie H, Muratore M, Bullion A, Lin G, Li H, Davis R, Lin X, Lakdawala AS, Cousins R, Field R, Payne J, Miller DD, Bamborough P, Christopher JA, Baldwin I, Osborn RR, Yonchuk J, Webb E, Rumsey WL. Kerns JK, et al. ACS Med Chem Lett. 2018 Oct 30;9(12):1164-1169. doi: 10.1021/acsmedchemlett.8b00291. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613320 Free PMC article.
Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IkappaB kinase-beta (IKK-beta).
Christopher JA, Bamborough P, Alder C, Campbell A, Cutler GJ, Down K, Hamadi AM, Jolly AM, Kerns JK, Lucas FS, Mellor GW, Miller DD, Morse MA, Pancholi KD, Rumsey W, Solanke YE, Williamson R. Christopher JA, et al. Among authors: kerns jk. J Med Chem. 2009 May 14;52(9):3098-102. doi: 10.1021/jm9000117. J Med Chem. 2009. PMID: 19348415
3,5-Disubstituted-indole-7-carboxamides: the discovery of a novel series of potent, selective inhibitors of IKK-β.
Miller DD, Bamborough P, Christopher JA, Baldwin IR, Champigny AC, Cutler GJ, Kerns JK, Longstaff T, Mellor GW, Morey JV, Morse MA, Nie H, Rumsey WL, Taggart JJ. Miller DD, et al. Among authors: kerns jk. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2255-8. doi: 10.1016/j.bmcl.2011.02.107. Epub 2011 Mar 1. Bioorg Med Chem Lett. 2011. PMID: 21429745
The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-alpha and IKK-beta kinases.
Christopher JA, Avitabile BG, Bamborough P, Champigny AC, Cutler GJ, Dyos SL, Grace KG, Kerns JK, Kitson JD, Mellor GW, Morey JV, Morse MA, O'Malley CF, Patel CB, Probst N, Rumsey W, Smith CA, Wilson MJ. Christopher JA, et al. Among authors: kerns jk. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3972-7. doi: 10.1016/j.bmcl.2007.04.088. Epub 2007 Apr 29. Bioorg Med Chem Lett. 2007. PMID: 17502144
Progress towards the development of anti-inflammatory inhibitors of IKKbeta.
Bamborough P, Callahan JF, Christopher JA, Kerns JK, Liddle J, Miller DD, Morse MA, Rumsey WL, Williamson R. Bamborough P, et al. Among authors: kerns jk. Curr Top Med Chem. 2009;9(7):623-39. doi: 10.2174/156802609789007336. Curr Top Med Chem. 2009. PMID: 19689370 Review.
Structure-Activity and Structure-Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein-Protein Interaction.
Heightman TD, Callahan JF, Chiarparin E, Coyle JE, Griffiths-Jones C, Lakdawala AS, McMenamin R, Mortenson PN, Norton D, Peakman TM, Rich SJ, Richardson C, Rumsey WL, Sanchez Y, Saxty G, Willems HMG, Wolfe L 3rd, Woolford AJ, Wu Z, Yan H, Kerns JK, Davies TG. Heightman TD, et al. Among authors: kerns jk. J Med Chem. 2019 May 9;62(9):4683-4702. doi: 10.1021/acs.jmedchem.9b00279. Epub 2019 Apr 25. J Med Chem. 2019. PMID: 30973731
Fragment-Guided Discovery of Pyrazole Carboxylic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2 Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction.
Norton D, Bonnette WG, Callahan JF, Carr MG, Griffiths-Jones CM, Heightman TD, Kerns JK, Nie H, Rich SJ, Richardson C, Rumsey W, Sanchez Y, Verdonk ML, Willems HMG, Wixted WE, Wolfe L 3rd, Woolford AJ, Wu Z, Davies TG. Norton D, et al. Among authors: kerns jk. J Med Chem. 2021 Nov 11;64(21):15949-15972. doi: 10.1021/acs.jmedchem.1c01351. Epub 2021 Oct 27. J Med Chem. 2021. PMID: 34705450
Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery.
Davies TG, Wixted WE, Coyle JE, Griffiths-Jones C, Hearn K, McMenamin R, Norton D, Rich SJ, Richardson C, Saxty G, Willems HM, Woolford AJ, Cottom JE, Kou JP, Yonchuk JG, Feldser HG, Sanchez Y, Foley JP, Bolognese BJ, Logan G, Podolin PL, Yan H, Callahan JF, Heightman TD, Kerns JK. Davies TG, et al. Among authors: kerns jk. J Med Chem. 2016 Apr 28;59(8):3991-4006. doi: 10.1021/acs.jmedchem.6b00228. Epub 2016 Apr 12. J Med Chem. 2016. PMID: 27031670
Discovery of a crystalline sulforaphane analog with good solid-state stability and engagement of the Nrf2 pathway in vitro and in vivo.
Boehm J, Davis R, Murar CE, Li T, McCleland B, Dong S, Yan H, Kerns J, Moody CJ, Wilson AJ, Graves AP, Mentzer M, Qi H, Yonchuk J, Kou JP, Foley J, Sanchez Y, Podolin PL, Bolognese B, Booth-Genthe C, Galop M, Wolfe L, Carr R, Callahan JF. Boehm J, et al. Bioorg Med Chem. 2019 Feb 15;27(4):579-588. doi: 10.1016/j.bmc.2018.12.026. Epub 2018 Dec 21. Bioorg Med Chem. 2019. PMID: 30626555
21 results