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Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.
Henry JR, Kaufman MD, Peng SB, Ahn YM, Caldwell TM, Vogeti L, Telikepalli H, Lu WP, Hood MM, Rutkoski TJ, Smith BD, Vogeti S, Miller D, Wise SC, Chun L, Zhang X, Zhang Y, Kays L, Hipskind PA, Wrobleski AD, Lobb KL, Clay JM, Cohen JD, Walgren JL, McCann D, Patel P, Clawson DK, Guo S, Manglicmot D, Groshong C, Logan C, Starling JJ, Flynn DL. Henry JR, et al. Among authors: hipskind pa. J Med Chem. 2015 May 28;58(10):4165-79. doi: 10.1021/acs.jmedchem.5b00067. Epub 2015 May 12. J Med Chem. 2015. PMID: 25965804
Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents.
Lobb KL, Hipskind PA, Aikins JA, Alvarez E, Cheung YY, Considine EL, De Dios A, Durst GL, Ferritto R, Grossman CS, Giera DD, Hollister BA, Huang Z, Iversen PW, Law KL, Li T, Lin HS, Lopez B, Lopez JE, Cabrejas LM, McCann DJ, Molero V, Reilly JE, Richett ME, Shih C, Teicher B, Wikel JH, White WT, Mader MM. Lobb KL, et al. Among authors: hipskind pa. J Med Chem. 2004 Oct 21;47(22):5367-80. doi: 10.1021/jm030594r. J Med Chem. 2004. PMID: 15481975
Potent and selective 1,2,3-trisubstituted indole NPY Y-1 antagonists.
Hipskind PA, Lobb KL, Nixon JA, Britton TC, Bruns RF, Catlow J, Dieckman-McGinty DK, Gackenheimer SL, Gitter BD, Iyengar S, Schober DA, Simmons RM, Swanson S, Zarrinmayeh H, Zimmerman DM, Gehlert DR. Hipskind PA, et al. J Med Chem. 1997 Nov 7;40(23):3712-4. doi: 10.1021/jm970512x. J Med Chem. 1997. PMID: 9371234 No abstract available.
3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.
Hipskind PA, Howbert JJ, Bruns RF, Cho SS, Crowell TA, Foreman MM, Gehlert DR, Iyengar S, Johnson KW, Krushinski JH, Li DL, Lobb KL, Mason NR, Muehl BS, Nixon JA, Phebus LA, Regoli D, Simmons RM, Threlkeld PG, Waters DC, Gitter BD. Hipskind PA, et al. J Med Chem. 1996 Feb 2;39(3):736-48. doi: 10.1021/jm950616c. J Med Chem. 1996. PMID: 8576917
Identification of Phenoxyalkylbenzimidazoles with Antitubercular Activity.
Chandrasekera NS, Alling T, Bailey MA, Files M, Early JV, Ollinger J, Ovechkina Y, Masquelin T, Desai PV, Cramer JW, Hipskind PA, Odingo JO, Parish T. Chandrasekera NS, et al. Among authors: hipskind pa. J Med Chem. 2015 Sep 24;58(18):7273-85. doi: 10.1021/acs.jmedchem.5b00546. Epub 2015 Sep 2. J Med Chem. 2015. PMID: 26295286
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