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Items: 1 to 50 of 64

1.

AMG 176, a Selective MCL1 Inhibitor, Is Effective in Hematologic Cancer Models Alone and in Combination with Established Therapies.

Caenepeel S, Brown SP, Belmontes B, Moody G, Keegan KS, Chui D, Whittington DA, Huang X, Poppe L, Cheng AC, Cardozo M, Houze J, Li Y, Lucas B, Paras NA, Wang X, Taygerly JP, Vimolratana M, Zancanella M, Zhu L, Cajulis E, Osgood T, Sun J, Damon L, Egan RK, Greninger P, McClanaghan JD, Gong J, Moujalled D, Pomilio G, Beltran P, Benes CH, Roberts AW, Huang DC, Wei A, Canon J, Coxon A, Hughes PE.

Cancer Discov. 2018 Dec;8(12):1582-1597. doi: 10.1158/2159-8290.CD-18-0387. Epub 2018 Sep 25. Erratum in: Cancer Discov. 2019 Jul;9(7):980.

PMID:
30254093
2.

Development of 2-aminooxazoline 3-azaxanthene β-amyloid cleaving enzyme (BACE) inhibitors with improved selectivity against Cathepsin D.

Low JD, Bartberger MD, Chen K, Cheng Y, Fielden MR, Gore V, Hickman D, Liu Q, Allen Sickmier E, Vargas HM, Werner J, White RD, Whittington DA, Wood S, Minatti AE.

Medchemcomm. 2017 Apr 27;8(6):1196-1206. doi: 10.1039/c7md00106a. eCollection 2017 Jun 1.

3.

Correction to Fragment-Linking Approach Using 19F NMR Spectroscopy To Obtain Highly Potent and Selective Inhibitors of β-Secretase.

Jordan JB, Whittington DA, Bartberger MD, Sickmier EA, Chen K, White RD, Cheng Y, Judd T.

J Med Chem. 2017 Apr 13;60(7):3218. doi: 10.1021/acs.jmedchem.7b00411. Epub 2017 Mar 28. No abstract available.

PMID:
28349692
4.

Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-1430).

Gonzalez-Lopez de Turiso F, Hao X, Shin Y, Bui M, Campuzano ID, Cardozo M, Dunn MC, Duquette J, Fisher B, Foti RS, Henne K, He X, Hu YL, Kelly RC, Johnson MG, Lucas BS, McCarter J, McGee LR, Medina JC, Metz D, San Miguel T, Mohn D, Tran T, Vissinga C, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang X, Cushing TD.

J Med Chem. 2016 Aug 11;59(15):7252-67. doi: 10.1021/acs.jmedchem.6b00827. Epub 2016 Jul 25.

PMID:
27411843
5.

Corrigendum to "Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling" [Bioorg. Med. Chem. 24 (2016) 2215-2234].

Liu L, Lee MR, Kim JL, Whittington DA, Bregman H, Hua Z, Lewis RT, Martin MW, Nishimura N, Potashman M, Yang K, Yi S, Vaida KR, Epstein LF, Babij C, Fernando M, Carnahan J, Norman MH.

Bioorg Med Chem. 2016 Jul 1;24(13):3093. doi: 10.1016/j.bmc.2016.05.014. Epub 2016 May 24. No abstract available.

PMID:
27234892
6.

Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling.

Liu L, Lee MR, Kim JL, Whittington DA, Bregman H, Hua Z, Lewis RT, Martin MW, Nishimura N, Potashman M, Yang K, Yi S, Vaida KR, Epstein LF, Babij C, Fernando M, Carnahan J, Norman MH.

Bioorg Med Chem. 2016 May 15;24(10):2215-34. doi: 10.1016/j.bmc.2016.03.055. Epub 2016 Apr 13. Erratum in: Bioorg Med Chem. 2016 Jul 1;24(13):3093.

PMID:
27085672
7.

Fragment-Linking Approach Using (19)F NMR Spectroscopy To Obtain Highly Potent and Selective Inhibitors of β-Secretase.

Jordan JB, Whittington DA, Bartberger MD, Sickmier EA, Chen K, Cheng Y, Judd T.

J Med Chem. 2016 Apr 28;59(8):3732-49. doi: 10.1021/acs.jmedchem.5b01917. Epub 2016 Apr 6. Erratum in: J Med Chem. 2017 Apr 13;60(7):3218.

PMID:
26978477
8.

Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity.

Boezio AA, Copeland KW, Rex K, K Albrecht B, Bauer D, Bellon SF, Boezio C, Broome MA, Choquette D, Coxon A, Dussault I, Hirai S, Lewis R, Lin MH, Lohman J, Liu J, Peterson EA, Potashman M, Shimanovich R, Teffera Y, Whittington DA, Vaida KR, Harmange JC.

J Med Chem. 2016 Mar 24;59(6):2328-42. doi: 10.1021/acs.jmedchem.5b01716. Epub 2016 Feb 11.

PMID:
26812066
9.

Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors.

Shin Y, Suchomel J, Cardozo M, Duquette J, He X, Henne K, Hu YL, Kelly RC, McCarter J, McGee LR, Medina JC, Metz D, San Miguel T, Mohn D, Tran T, Vissinga C, Wong S, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang X, Cushing TD.

J Med Chem. 2016 Jan 14;59(1):431-47. doi: 10.1021/acs.jmedchem.5b01651. Epub 2015 Dec 21.

PMID:
26652588
10.

The imidazo[1,2-a]pyridine ring system as a scaffold for potent dual phosphoinositide-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitors.

Stec MM, Andrews KL, Bo Y, Caenepeel S, Liao H, McCarter J, Mullady EL, San Miguel T, Subramanian R, Tamayo N, Whittington DA, Wang L, Wu T, Zalameda LP, Zhang N, Hughes PE, Norman MH.

Bioorg Med Chem Lett. 2015 Oct 1;25(19):4136-42. doi: 10.1016/j.bmcl.2015.08.016. Epub 2015 Aug 8.

PMID:
26298499
11.

Correction to Discovery of Potent and Selective 8-Fluorotriazolopyridine c-Met Inhibitors.

Peterson EA, Teffera Y, Albrecht BK, Bauer D, Bellon SF, Boezio A, Boezio C, Broome MA, Choquette D, Copeland KW, Dussault I, Lewis R, Lin MH, Lohman J, Liu J, Potashman M, Rex K, Shimanovich R, Whittington DA, Vaida KR, Harmange JC.

J Med Chem. 2015 May 14;58(9):4087. doi: 10.1021/acs.jmedchem.5b00591. Epub 2015 Apr 22. No abstract available.

PMID:
25901648
12.

Discovery of potent and selective 8-fluorotriazolopyridine c-Met inhibitors.

Peterson EA, Teffera Y, Albrecht BK, Bauer D, Bellon SF, Boezio A, Boezio C, Broome MA, Choquette D, Copeland KW, Dussault I, Lewis R, Lin MH, Lohman J, Liu J, Potashman M, Rex K, Shimanovich R, Whittington DA, Vaida KR, Harmange JC.

J Med Chem. 2015 Mar 12;58(5):2417-30. doi: 10.1021/jm501913a. Epub 2015 Mar 3. Erratum in: J Med Chem. 2015 May 14;58(9):4087.

PMID:
25699405
13.

An Orally Available BACE1 Inhibitor That Affords Robust CNS Aβ Reduction without Cardiovascular Liabilities.

Cheng Y, Brown J, Judd TC, Lopez P, Qian W, Powers TS, Chen JJ, Bartberger MD, Chen K, Dunn RT 2nd, Epstein O, Fremeau RT Jr, Harried S, Hickman D, Hitchcock SA, Luo Y, Minatti AE, Patel VF, Vargas HM, Wahl RC, Weiss MM, Wen PH, White RD, Whittington DA, Zheng XM, Wood S.

ACS Med Chem Lett. 2014 Dec 29;6(2):210-5. doi: 10.1021/ml500458t. eCollection 2015 Feb 12.

14.

Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer's disease.

Chen JJ, Liu Q, Yuan C, Gore V, Lopez P, Ma V, Amegadzie A, Qian W, Judd TC, Minatti AE, Brown J, Cheng Y, Xue M, Zhong W, Dineen TA, Epstein O, Human J, Kreiman C, Marx I, Weiss MM, Hitchcock SA, Powers TS, Chen K, Wen PH, Whittington DA, Cheng AC, Bartberger MD, Hickman D, Werner JA, Vargas HM, Everds NE, Vonderfecht SL, Dunn RT 2nd, Wood S, Fremeau RT Jr, White RD, Patel VF.

Bioorg Med Chem Lett. 2015 Feb 15;25(4):767-74. doi: 10.1016/j.bmcl.2014.12.092. Epub 2015 Jan 8.

PMID:
25613679
15.

Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease.

Cushing TD, Hao X, Shin Y, Andrews K, Brown M, Cardozo M, Chen Y, Duquette J, Fisher B, Gonzalez-Lopez de Turiso F, He X, Henne KR, Hu YL, Hungate R, Johnson MG, Kelly RC, Lucas B, McCarter JD, McGee LR, Medina JC, San Miguel T, Mohn D, Pattaropong V, Pettus LH, Reichelt A, Rzasa RM, Seganish J, Tasker AS, Wahl RC, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang D, Metz DP.

J Med Chem. 2015 Jan 8;58(1):480-511. doi: 10.1021/jm501624r. Epub 2014 Dec 3.

PMID:
25469863
16.

Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511.

Lanman BA, Reed AB, Cee VJ, Hong FT, Pettus LH, Wurz RP, Andrews KL, Jiang J, McCarter JD, Mullady EL, San Miguel T, Subramanian R, Wang L, Whittington DA, Wu T, Zalameda L, Zhang N, Tasker AS, Hughes PE, Norman MH.

Bioorg Med Chem Lett. 2014 Dec 15;24(24):5630-5634. doi: 10.1016/j.bmcl.2014.10.085. Epub 2014 Nov 1.

PMID:
25466188
17.

Lead optimization and modulation of hERG activity in a series of aminooxazoline xanthene β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.

Epstein O, Bryan MC, Cheng AC, Derakhchan K, Dineen TA, Hickman D, Hua Z, Human JB, Kreiman C, Marx IE, Weiss MM, Wahl RC, Wen PH, Whittington DA, Wood S, Zheng XM, Fremeau RT Jr, White RD, Patel VF.

J Med Chem. 2014 Dec 11;57(23):9796-810. doi: 10.1021/jm501266w. Epub 2014 Nov 12.

PMID:
25389560
18.

Inhibitors of β-site amyloid precursor protein cleaving enzyme (BACE1): identification of (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine (AMG-8718).

Dineen TA, Chen K, Cheng AC, Derakhchan K, Epstein O, Esmay J, Hickman D, Kreiman CE, Marx IE, Wahl RC, Wen PH, Weiss MM, Whittington DA, Wood S, Fremeau RT Jr, White RD, Patel VF.

J Med Chem. 2014 Dec 11;57(23):9811-31. doi: 10.1021/jm5012676. Epub 2014 Nov 14.

PMID:
25363711
19.

Hydroxyethylamine-based inhibitors of BACE1: P₁-P₃ macrocyclization can improve potency, selectivity, and cell activity.

Pennington LD, Whittington DA, Bartberger MD, Jordan SR, Monenschein H, Nguyen TT, Yang BH, Xue QM, Vounatsos F, Wahl RC, Chen K, Wood S, Citron M, Patel VF, Hitchcock SA, Zhong W.

Bioorg Med Chem Lett. 2013 Aug 1;23(15):4459-64. doi: 10.1016/j.bmcl.2013.05.028. Epub 2013 May 16.

PMID:
23769639
20.

The R1275Q neuroblastoma mutant and certain ATP-competitive inhibitors stabilize alternative activation loop conformations of anaplastic lymphoma kinase.

Epstein LF, Chen H, Emkey R, Whittington DA.

J Biol Chem. 2012 Oct 26;287(44):37447-57. doi: 10.1074/jbc.M112.391425. Epub 2012 Aug 29.

21.

Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer's disease.

Huang H, La DS, Cheng AC, Whittington DA, Patel VF, Chen K, Dineen TA, Epstein O, Graceffa R, Hickman D, Kiang YH, Louie S, Luo Y, Wahl RC, Wen PH, Wood S, Fremeau RT Jr.

J Med Chem. 2012 Nov 8;55(21):9156-69. doi: 10.1021/jm300598e. Epub 2012 Sep 11.

PMID:
22928914
22.

PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases.

Cushing TD, Metz DP, Whittington DA, McGee LR.

J Med Chem. 2012 Oct 25;55(20):8559-81. doi: 10.1021/jm300847w. Epub 2012 Sep 13. Review. No abstract available.

PMID:
22924688
23.

Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511.

Norman MH, Andrews KL, Bo YY, Booker SK, Caenepeel S, Cee VJ, D'Angelo ND, Freeman DJ, Herberich BJ, Hong FT, Jackson CL, Jiang J, Lanman BA, Liu L, McCarter JD, Mullady EL, Nishimura N, Pettus LH, Reed AB, Miguel TS, Smith AL, Stec MM, Tadesse S, Tasker A, Aidasani D, Zhu X, Subramanian R, Tamayo NA, Wang L, Whittington DA, Wu B, Wu T, Wurz RP, Yang K, Zalameda L, Zhang N, Hughes PE.

J Med Chem. 2012 Sep 13;55(17):7796-816. doi: 10.1021/jm300846z. Epub 2012 Aug 30. Erratum in: J Med Chem. 2012 Oct 25;55(20):8975.

PMID:
22897589
24.

Discovery and in vivo evaluation of dual PI3Kβ/δ inhibitors.

Gonzalez-Lopez de Turiso F, Shin Y, Brown M, Cardozo M, Chen Y, Fong D, Hao X, He X, Henne K, Hu YL, Johnson MG, Kohn T, Lohman J, McBride HJ, McGee LR, Medina JC, Metz D, Miner K, Mohn D, Pattaropong V, Seganish J, Simard JL, Wannberg S, Whittington DA, Yu G, Cushing TD.

J Med Chem. 2012 Sep 13;55(17):7667-85. doi: 10.1021/jm300679u. Epub 2012 Aug 29.

PMID:
22876881
25.

Synthesis and structure-activity relationships of dual PI3K/mTOR inhibitors based on a 4-amino-6-methyl-1,3,5-triazine sulfonamide scaffold.

Wurz RP, Liu L, Yang K, Nishimura N, Bo Y, Pettus LH, Caenepeel S, Freeman DJ, McCarter JD, Mullady EL, Miguel TS, Wang L, Zhang N, Andrews KL, Whittington DA, Jiang J, Subramanian R, Hughes PE, Norman MH.

Bioorg Med Chem Lett. 2012 Sep 1;22(17):5714-20. doi: 10.1016/j.bmcl.2012.06.078. Epub 2012 Jul 3.

PMID:
22832322
26.

The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.

Lewis RT, Bode CM, Choquette DM, Potashman M, Romero K, Stellwagen JC, Teffera Y, Moore E, Whittington DA, Chen H, Epstein LF, Emkey R, Andrews PS, Yu VL, Saffran DC, Xu M, Drew A, Merkel P, Szilvassy S, Brake RL.

J Med Chem. 2012 Jul 26;55(14):6523-40. doi: 10.1021/jm3005866. Epub 2012 Jul 10.

PMID:
22734674
27.

Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors.

Bode CM, Boezio AA, Albrecht BK, Bellon SF, Berry L, Broome MA, Choquette D, Dussault I, Lewis RT, Lin MH, Rex K, Whittington DA, Yang Y, Harmange JC.

Bioorg Med Chem Lett. 2012 Jun 15;22(12):4089-93. doi: 10.1016/j.bmcl.2012.04.072. Epub 2012 Apr 25.

PMID:
22595176
28.

Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases.

Smith AL, D'Angelo ND, Bo YY, Booker SK, Cee VJ, Herberich B, Hong FT, Jackson CL, Lanman BA, Liu L, Nishimura N, Pettus LH, Reed AB, Tadesse S, Tamayo NA, Wurz RP, Yang K, Andrews KL, Whittington DA, McCarter JD, Miguel TS, Zalameda L, Jiang J, Subramanian R, Mullady EL, Caenepeel S, Freeman DJ, Wang L, Zhang N, Wu T, Hughes PE, Norman MH.

J Med Chem. 2012 Jun 14;55(11):5188-219. doi: 10.1021/jm300184s. Epub 2012 May 23.

PMID:
22548365
29.

Design and synthesis of potent, orally efficacious hydroxyethylamine derived β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.

Dineen TA, Weiss MM, Williamson T, Acton P, Babu-Khan S, Bartberger MD, Brown J, Chen K, Cheng Y, Citron M, Croghan MD, Dunn RT 2nd, Esmay J, Graceffa RF, Harried SS, Hickman D, Hitchcock SA, Horne DB, Huang H, Imbeah-Ampiah R, Judd T, Kaller MR, Kreiman CR, La DS, Li V, Lopez P, Louie S, Monenschein H, Nguyen TT, Pennington LD, San Miguel T, Sickmier EA, Vargas HM, Wahl RC, Wen PH, Whittington DA, Wood S, Xue Q, Yang BH, Patel VF, Zhong W.

J Med Chem. 2012 Nov 8;55(21):9025-44. doi: 10.1021/jm300118s. Epub 2012 Apr 18.

PMID:
22468684
30.

Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.

Liu L, Norman MH, Lee M, Xi N, Siegmund A, Boezio AA, Booker S, Choquette D, D'Angelo ND, Germain J, Yang K, Yang Y, Zhang Y, Bellon SF, Whittington DA, Harmange JC, Dominguez C, Kim TS, Dussault I.

J Med Chem. 2012 Mar 8;55(5):1868-97. doi: 10.1021/jm201331s. Epub 2012 Feb 24.

PMID:
22320327
31.

Rapid development of piperidine carboxamides as potent and selective anaplastic lymphoma kinase inhibitors.

Bryan MC, Whittington DA, Doherty EM, Falsey JR, Cheng AC, Emkey R, Brake RL, Lewis RT.

J Med Chem. 2012 Feb 23;55(4):1698-705. doi: 10.1021/jm201565s. Epub 2012 Feb 9.

PMID:
22263917
32.

Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives.

Nishimura N, Siegmund A, Liu L, Yang K, Bryan MC, Andrews KL, Bo Y, Booker SK, Caenepeel S, Freeman D, Liao H, McCarter J, Mullady EL, San Miguel T, Subramanian R, Tamayo N, Wang L, Whittington DA, Zalameda L, Zhang N, Hughes PE, Norman MH.

J Med Chem. 2011 Jul 14;54(13):4735-51. doi: 10.1021/jm200386s. Epub 2011 Jun 20.

PMID:
21612232
33.

Discovery of triazine-benzimidazoles as selective inhibitors of mTOR.

Peterson EA, Andrews PS, Be X, Boezio AA, Bush TL, Cheng AC, Coats JR, Colletti AE, Copeland KW, DuPont M, Graceffa R, Grubinska B, Harmange JC, Kim JL, Mullady EL, Olivieri P, Schenkel LB, Stanton MK, Teffera Y, Whittington DA, Cai T, La DS.

Bioorg Med Chem Lett. 2011 Apr 1;21(7):2064-70. doi: 10.1016/j.bmcl.2011.02.007. Epub 2011 Feb 12.

PMID:
21376583
34.

Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.

D'Angelo ND, Kim TS, Andrews K, Booker SK, Caenepeel S, Chen K, D'Amico D, Freeman D, Jiang J, Liu L, McCarter JD, San Miguel T, Mullady EL, Schrag M, Subramanian R, Tang J, Wahl RC, Wang L, Whittington DA, Wu T, Xi N, Xu Y, Yakowec P, Yang K, Zalameda LP, Zhang N, Hughes P, Norman MH.

J Med Chem. 2011 Mar 24;54(6):1789-811. doi: 10.1021/jm1014605. Epub 2011 Feb 18.

PMID:
21332118
35.

Structure of prokaryotic polyamine deacetylase reveals evolutionary functional relationships with eukaryotic histone deacetylases.

Lombardi PM, Angell HD, Whittington DA, Flynn EF, Rajashankar KR, Christianson DW.

Biochemistry. 2011 Mar 22;50(11):1808-17. doi: 10.1021/bi101859k. Epub 2011 Jan 26.

36.

Selective inhibitors of the mutant B-Raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline.

Smith AL, DeMorin FF, Paras NA, Huang Q, Petkus JK, Doherty EM, Nixey T, Kim JL, Whittington DA, Epstein LF, Lee MR, Rose MJ, Babij C, Fernando M, Hess K, Le Q, Beltran P, Carnahan J.

J Med Chem. 2009 Oct 22;52(20):6189-92. doi: 10.1021/jm901081g.

PMID:
19764794
37.

Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase.

Cee VJ, Cheng AC, Romero K, Bellon S, Mohr C, Whittington DA, Bak A, Bready J, Caenepeel S, Coxon A, Deak HL, Fretland J, Gu Y, Hodous BL, Huang X, Kim JL, Lin J, Long AM, Nguyen H, Olivieri PR, Patel VF, Wang L, Zhou Y, Hughes P, Geuns-Meyer S.

Bioorg Med Chem Lett. 2009 Jan 15;19(2):424-7. doi: 10.1016/j.bmcl.2008.11.056. Epub 2008 Nov 20.

PMID:
19062275
38.

Discovery of amido-benzisoxazoles as potent c-Kit inhibitors.

Kunz RK, Rumfelt S, Chen N, Zhang D, Tasker AS, Bürli R, Hungate R, Yu V, Nguyen Y, Whittington DA, Meagher KL, Plant M, Tudor Y, Schrag M, Xu Y, Ng GY, Hu E.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5115-7. doi: 10.1016/j.bmcl.2008.07.111. Epub 2008 Jul 31.

PMID:
18723346
39.

Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.

Bauer D, Whittington DA, Coxon A, Bready J, Harriman SP, Patel VF, Polverino A, Harmange JC.

Bioorg Med Chem Lett. 2008 Sep 1;18(17):4844-8. doi: 10.1016/j.bmcl.2008.07.080. Epub 2008 Jul 24.

PMID:
18682324
40.

Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit.

Hu E, Tasker A, White RD, Kunz RK, Human J, Chen N, Bürli R, Hungate R, Novak P, Itano A, Zhang X, Yu V, Nguyen Y, Tudor Y, Plant M, Flynn S, Xu Y, Meagher KL, Whittington DA, Ng GY.

J Med Chem. 2008 Jun 12;51(11):3065-8. doi: 10.1021/jm800188g. Epub 2008 May 1.

PMID:
18447379
41.

Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.

Harmange JC, Weiss MM, Germain J, Polverino AJ, Borg G, Bready J, Chen D, Choquette D, Coxon A, DeMelfi T, DiPietro L, Doerr N, Estrada J, Flynn J, Graceffa RF, Harriman SP, Kaufman S, La DS, Long A, Martin MW, Neervannan S, Patel VF, Potashman M, Regal K, Roveto PM, Schrag ML, Starnes C, Tasker A, Teffera Y, Wang L, White RD, Whittington DA, Zanon R.

J Med Chem. 2008 Mar 27;51(6):1649-67. doi: 10.1021/jm701097z. Epub 2008 Mar 7.

PMID:
18324761
42.

Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors.

Weiss MM, Harmange JC, Polverino AJ, Bauer D, Berry L, Berry V, Borg G, Bready J, Chen D, Choquette D, Coxon A, DeMelfi T, Doerr N, Estrada J, Flynn J, Graceffa RF, Harriman SP, Kaufman S, La DS, Long A, Neervannan S, Patel VF, Potashman M, Regal K, Roveto PM, Schrag ML, Starnes C, Tasker A, Teffera Y, Whittington DA, Zanon R.

J Med Chem. 2008 Mar 27;51(6):1668-80. doi: 10.1021/jm701098w. Epub 2008 Mar 7.

PMID:
18324759
43.

Novel 2,3-dihydro-1,4-benzoxazines as potent and orally bioavailable inhibitors of tumor-driven angiogenesis.

La DS, Belzile J, Bready JV, Coxon A, DeMelfi T, Doerr N, Estrada J, Flynn JC, Flynn SR, Graceffa RF, Harriman SP, Larrow JF, Long AM, Martin MW, Morrison MJ, Patel VF, Roveto PM, Wang L, Weiss MM, Whittington DA, Teffera Y, Zhao Z, Polverino AJ, Harmange JC.

J Med Chem. 2008 Mar 27;51(6):1695-705. doi: 10.1021/jm701129j. Epub 2008 Feb 27.

PMID:
18311900
44.

Amphipathic benzoic acid derivatives: synthesis and binding in the hydrophobic tunnel of the zinc deacetylase LpxC.

Shin H, Gennadios HA, Whittington DA, Christianson DW.

Bioorg Med Chem. 2007 Apr 1;15(7):2617-23. Epub 2007 Jan 31.

PMID:
17296300
45.

Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor.

Hodous BL, Geuns-Meyer SD, Hughes PE, Albrecht BK, Bellon S, Bready J, Caenepeel S, Cee VJ, Chaffee SC, Coxon A, Emery M, Fretland J, Gallant P, Gu Y, Hoffman D, Johnson RE, Kendall R, Kim JL, Long AM, Morrison M, Olivieri PR, Patel VF, Polverino A, Rose P, Tempest P, Wang L, Whittington DA, Zhao H.

J Med Chem. 2007 Feb 22;50(4):611-26. Epub 2007 Jan 25.

PMID:
17253678
46.

Mechanistic inferences from the binding of ligands to LpxC, a metal-dependent deacetylase.

Gennadios HA, Whittington DA, Li X, Fierke CA, Christianson DW.

Biochemistry. 2006 Jul 4;45(26):7940-8.

47.

UDP-3-O-((R)-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase functions through a general acid-base catalyst pair mechanism.

Hernick M, Gennadios HA, Whittington DA, Rusche KM, Christianson DW, Fierke CA.

J Biol Chem. 2005 Apr 29;280(17):16969-78. Epub 2005 Feb 10.

48.

Expression, assay, and structure of the extracellular domain of murine carbonic anhydrase XIV: implications for selective inhibition of membrane-associated isozymes.

Whittington DA, Grubb JH, Waheed A, Shah GN, Sly WS, Christianson DW.

J Biol Chem. 2004 Feb 20;279(8):7223-8. Epub 2003 Dec 3.

49.

Crystal structure of LpxC, a zinc-dependent deacetylase essential for endotoxin biosynthesis.

Whittington DA, Rusche KM, Shin H, Fierke CA, Christianson DW.

Proc Natl Acad Sci U S A. 2003 Jul 8;100(14):8146-50. Epub 2003 Jun 20.

50.

Bornyl diphosphate synthase: structure and strategy for carbocation manipulation by a terpenoid cyclase.

Whittington DA, Wise ML, Urbansky M, Coates RM, Croteau RB, Christianson DW.

Proc Natl Acad Sci U S A. 2002 Nov 26;99(24):15375-80. Epub 2002 Nov 13.

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