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101 results

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Page 1
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
Moffett K, Konteatis Z, Nguyen D, Shetty R, Ludington J, Fujimoto T, Lee KJ, Chai X, Namboodiri H, Karpusas M, Dorsey B, Guarnieri F, Bukhtiyarova M, Springman E, Michelotti E. Moffett K, et al. Among authors: dorsey b. Bioorg Med Chem Lett. 2011 Dec 1;21(23):7155-65. doi: 10.1016/j.bmcl.2011.09.078. Epub 2011 Sep 28. Bioorg Med Chem Lett. 2011. PMID: 22014550
L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.
Sanderson PE, Cutrona KJ, Dorsey BD, Dyer DL, McDonough CM, Naylor-Olsen AM, Chen IW, Chen Z, Cook JJ, Gardell SJ, Krueger JA, Lewis SD, Lin JH, Lucas BJ Jr, Lyle EA, Lynch JJ Jr, Stranieri MT, Vastag K, Shafer JA, Vacca JP. Sanderson PE, et al. Among authors: dorsey bd. Bioorg Med Chem Lett. 1998 Apr 7;8(7):817-22. doi: 10.1016/s0960-894x(98)00117-6. Bioorg Med Chem Lett. 1998. PMID: 9871547
Synthesis and pharmacological evaluation of N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent.
Shetty RS, Lee Y, Liu B, Husain A, Joseph RW, Lu Y, Nelson D, Mihelcic J, Chao W, Moffett KK, Schumacher A, Flubacher D, Stojanovic A, Bukhtiyarova M, Williams K, Lee KJ, Ochman AR, Saporito MS, Moore WR, Flynn GA, Dorsey BD, Springman EB, Fujimoto T, Kelly MJ. Shetty RS, et al. Among authors: dorsey bd. J Med Chem. 2011 Jan 13;54(1):179-200. doi: 10.1021/jm100659v. Epub 2010 Dec 2. J Med Chem. 2011. PMID: 21126027
P3 optimization of functional potency, in vivo efficacy and oral bioavailability in 3-aminopyrazinone thrombin inhibitors bearing non-charged groups at the P1 position.
Isaacs RC, Newton CL, Cutrona KJ, Mercer SP, Dorsey BD, McDonough CM, Cook JJ, Krueger JA, Lewis SD, Lucas BJ, Lyle EA, Lynch JJ, Miller-Stein C, Michener MT, Wallace AA, White RB, Wong BK. Isaacs RC, et al. Among authors: dorsey bd. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1532-5. doi: 10.1016/j.bmcl.2010.12.108. Epub 2010 Dec 28. Bioorg Med Chem Lett. 2011. PMID: 21295466
4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors.
Holladay MW, Campbell BT, Rowbottom MW, Chao Q, Sprankle KG, Lai AG, Abraham S, Setti E, Faraoni R, Tran L, Armstrong RC, Gunawardane RN, Gardner MF, Cramer MD, Gitnick D, Ator MA, Dorsey BD, Ruggeri BR, Williams M, Bhagwat SS, James J. Holladay MW, et al. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5342-6. doi: 10.1016/j.bmcl.2011.07.019. Epub 2011 Jul 14. Bioorg Med Chem Lett. 2011. PMID: 21807507
Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models.
Mesaros EF, Burke JP, Parrish JD, Dugan BJ, Anzalone AV, Angeles TS, Albom MS, Aimone LD, Quail MR, Wan W, Lu L, Huang Z, Ator MA, Ruggeri BA, Cheng M, Ott GR, Dorsey BD. Mesaros EF, et al. Bioorg Med Chem Lett. 2011 Jan 1;21(1):463-6. doi: 10.1016/j.bmcl.2010.10.115. Epub 2010 Oct 27. Bioorg Med Chem Lett. 2011. PMID: 21074994
101 results