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Page 1
Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors.
Abraham S, Hadd MJ, Tran L, Vickers T, Sindac J, Milanov ZV, Holladay MW, Bhagwat SS, Hua H, Ford Pulido JM, Cramer MD, Gitnick D, James J, Dao A, Belli B, Armstrong RC, Treiber DK, Liu G. Abraham S, et al. Among authors: holladay mw. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5296-300. doi: 10.1016/j.bmcl.2011.07.027. Epub 2011 Jul 14. Bioorg Med Chem Lett. 2011. PMID: 21802948
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
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.
Rowbottom MW, Faraoni R, Chao Q, Campbell BT, Lai AG, Setti E, Ezawa M, Sprankle KG, Abraham S, Tran L, Struss B, Gibney M, Armstrong RC, Gunawardane RN, Nepomuceno RR, Valenta I, Hua H, Gardner MF, Cramer MD, Gitnick D, Insko DE, Apuy JL, Jones-Bolin S, Ghose AK, Herbertz T, Ator MA, Dorsey BD, Ruggeri B, Williams M, Bhagwat S, James J, Holladay MW. Rowbottom MW, et al. Among authors: holladay mw. J Med Chem. 2012 Feb 9;55(3):1082-105. doi: 10.1021/jm2009925. Epub 2012 Jan 23. J Med Chem. 2012. PMID: 22168626
Discovery of highly potent and selective pan-Aurora kinase inhibitors with enhanced in vivo antitumor therapeutic index.
Liu G, Abraham S, Tran L, Vickers TD, Xu S, Hadd MJ, Quiambao S, Holladay MW, Hua H, Ford Pulido JM, Gunawardane RN, Davis MI, Eichelberger SR, Apuy JL, Gitnick D, Gardner MF, James J, Breider MA, Belli B, Armstrong RC, Treiber DK. Liu G, et al. Among authors: holladay mw. J Med Chem. 2012 Apr 12;55(7):3250-60. doi: 10.1021/jm201702g. Epub 2012 Mar 14. J Med Chem. 2012. PMID: 22380736
Discovery and optimization of a highly efficacious class of 5-aryl-2-aminopyridines as FMS-like tyrosine kinase 3 (FLT3) inhibitors.
Liu G, Abraham S, Liu X, Xu S, Rooks AM, Nepomuceno R, Dao A, Brigham D, Gitnick D, Insko DE, Gardner MF, Zarrinkar PP, Christopher R, Belli B, Armstrong RC, Holladay MW. Liu G, et al. Among authors: holladay mw. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3436-41. doi: 10.1016/j.bmcl.2015.07.023. Epub 2015 Jul 14. Bioorg Med Chem Lett. 2015. PMID: 26208887
CEP-32496: a novel orally active BRAF(V600E) inhibitor with selective cellular and in vivo antitumor activity.
James J, Ruggeri B, Armstrong RC, Rowbottom MW, Jones-Bolin S, Gunawardane RN, Dobrzanski P, Gardner MF, Zhao H, Cramer MD, Hunter K, Nepomuceno RR, Cheng M, Gitnick D, Yazdanian M, Insko DE, Ator MA, Apuy JL, Faraoni R, Dorsey BD, Williams M, Bhagwat SS, Holladay MW. James J, et al. Among authors: holladay mw. Mol Cancer Ther. 2012 Apr;11(4):930-41. doi: 10.1158/1535-7163.MCT-11-0645. Epub 2012 Feb 7. Mol Cancer Ther. 2012. PMID: 22319199
Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent: effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice.
Holladay MW, Bai H, Li Y, Lin NH, Daanen JF, Ryther KB, Wasicak JT, Kincaid JF, He Y, Hettinger AM, Huang P, Anderson DJ, Bannon AW, Buckley MJ, Campbell JE, Donnelly-Roberts DL, Gunther KL, Kim DJ, Kuntzweiler TA, Sullivan JP, Decker MW, Arneric SP. Holladay MW, et al. Bioorg Med Chem Lett. 1998 Oct 6;8(19):2797-802. doi: 10.1016/s0960-894x(98)00504-6. Bioorg Med Chem Lett. 1998. PMID: 9873625
Synthesis and structure-activity relationships of pyridine-modified analogs of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine, A-84543, a potent nicotinic acetylcholine receptor agonist.
Lin NH, Gunn DE, Li Y, He Y, Bai H, Ryther KB, Kuntzweiler T, Donnelly-Roberts DL, Anderson DJ, Campbell JE, Sullivan JP, Arneric SP, Holladay MW. Lin NH, et al. Among authors: holladay mw. Bioorg Med Chem Lett. 1998 Feb 3;8(3):249-54. doi: 10.1016/s0960-894x(98)00019-5. Bioorg Med Chem Lett. 1998. PMID: 9871663
Synthesis and structure-activity relationships of a novel series of 2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide K(ATP) channel openers: discovery of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9- hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637), a potent K(ATP) opener that selectively inhibits spontaneous bladder contractions.
Carroll WA, Altenbach RJ, Bai H, Brioni JD, Brune ME, Buckner SA, Cassidy C, Chen Y, Coghlan MJ, Daza AV, Drizin I, Fey TA, Fitzgerald M, Gopalakrishnan M, Gregg RJ, Henry RF, Holladay MW, King LL, Kort ME, Kym PR, Milicic I, Tang R, Turner SC, Whiteaker KL, Yi L, Zhang H, Sullivan JP. Carroll WA, et al. Among authors: holladay mw. J Med Chem. 2004 Jun 3;47(12):3163-79. doi: 10.1021/jm030356w. J Med Chem. 2004. PMID: 15163196
46 results