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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: walgren jl. 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
Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers.
Peng SB, Henry JR, Kaufman MD, Lu WP, Smith BD, Vogeti S, Rutkoski TJ, Wise S, Chun L, Zhang Y, Van Horn RD, Yin T, Zhang X, Yadav V, Chen SH, Gong X, Ma X, Webster Y, Buchanan S, Mochalkin I, Huber L, Kays L, Donoho GP, Walgren J, McCann D, Patel P, Conti I, Plowman GD, Starling JJ, Flynn DL. Peng SB, et al. Cancer Cell. 2015 Sep 14;28(3):384-98. doi: 10.1016/j.ccell.2015.08.002. Epub 2015 Sep 3. Cancer Cell. 2015. PMID: 26343583 Free article.
ERK Inhibitor LY3214996 Targets ERK Pathway-Driven Cancers: A Therapeutic Approach Toward Precision Medicine.
Bhagwat SV, McMillen WT, Cai S, Zhao B, Whitesell M, Shen W, Kindler L, Flack RS, Wu W, Anderson B, Zhai Y, Yuan XJ, Pogue M, Van Horn RD, Rao X, McCann D, Dropsey AJ, Manro J, Walgren J, Yuen E, Rodriguez MJ, Plowman GD, Tiu RV, Joseph S, Peng SB. Bhagwat SV, et al. Mol Cancer Ther. 2020 Feb;19(2):325-336. doi: 10.1158/1535-7163.MCT-19-0183. Epub 2019 Nov 19. Mol Cancer Ther. 2020. PMID: 31744895
Aurora A-Selective Inhibitor LY3295668 Leads to Dominant Mitotic Arrest, Apoptosis in Cancer Cells, and Shows Potent Preclinical Antitumor Efficacy.
Du J, Yan L, Torres R, Gong X, Bian H, Marugán C, Boehnke K, Baquero C, Hui YH, Chapman SC, Yang Y, Zeng Y, Bogner SM, Foreman RT, Capen A, Donoho GP, Van Horn RD, Barnard DS, Dempsey JA, Beckmann RP, Marshall MS, Chio LC, Qian Y, Webster YW, Aggarwal A, Chu S, Bhattachar S, Stancato LF, Dowless MS, Iversen PW, Manro JR, Walgren JL, Halstead BW, Dieter MZ, Martinez R, Bhagwat SV, Kreklau EL, Lallena MJ, Ye XS, Patel BKR, Reinhard C, Plowman GD, Barda DA, Henry JR, Buchanan SG, Campbell RM. Du J, et al. Among authors: walgren jl. Mol Cancer Ther. 2019 Dec;18(12):2207-2219. doi: 10.1158/1535-7163.MCT-18-0529. Epub 2019 Sep 17. Mol Cancer Ther. 2019. PMID: 31530649
Design, synthesis, and biological evaluation of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one, a potent, orally active, brain penetrant inhibitor of phosphodiesterase 5 (PDE5).
Hughes RO, Rogier DJ, Jacobsen EJ, Walker JK, Macinnes A, Bond BR, Zhang LL, Yu Y, Zheng Y, Rumsey JM, Walgren JL, Curtiss SW, Fobian YM, Heasley SE, Cubbage JW, Moon JB, Brown DL, Acker BA, Maddux TM, Tollefson MB, Mischke BV, Owen DR, Freskos JN, Molyneaux JM, Benson AG, Blevis-Bal RM. Hughes RO, et al. Among authors: walgren jl. J Med Chem. 2010 Mar 25;53(6):2656-60. doi: 10.1021/jm901781q. J Med Chem. 2010. PMID: 20196613
18 results