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Items: 27

1.

Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).

Rew Y, Du X, Eksterowicz J, Zhou H, Jahchan N, Zhu L, Yan X, Kawai H, McGee LR, Medina JC, Huang T, Chen C, Zavorotinskaya T, Sutimantanapi D, Waszczuk J, Jackson E, Huang E, Ye Q, Fantin VR, Sun D.

J Med Chem. 2018 Sep 13;61(17):7767-7784. doi: 10.1021/acs.jmedchem.8b00743. Epub 2018 Aug 23.

PMID:
30091920
2.

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
3.

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
4.

Synthesis and SAR study of potent and selective PI3Kδ inhibitors.

Bui M, Hao X, Shin Y, Cardozo M, He X, Henne K, Suchomel J, McCarter J, McGee LR, San Miguel T, Medina JC, Mohn D, Tran T, Wannberg S, Wong J, Wong S, Zalameda L, Metz D, Cushing TD.

Bioorg Med Chem Lett. 2015 Mar 1;25(5):1104-9. doi: 10.1016/j.bmcl.2015.01.001. Epub 2015 Jan 17.

PMID:
25666823
5.

AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia.

Li C, Liu L, Liang L, Xia Z, Li Z, Wang X, McGee LR, Newhall K, Sinclair A, Kamb A, Wickramasinghe D, Dai K.

Mol Cancer Ther. 2015 Feb;14(2):375-83. doi: 10.1158/1535-7163.MCT-14-0388. Epub 2014 Dec 8.

6.

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
7.

Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction.

Rew Y, Sun D, Yan X, Beck HP, Canon J, Chen A, Duquette J, Eksterowicz J, Fox BM, Fu J, Gonzalez AZ, Houze J, Huang X, Jiang M, Jin L, Li Y, Li Z, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, Oliner JD, Osgood T, Saiki AY, Shaffer P, Wang YC, Wortman S, Yakowec P, Ye Q, Yu D, Zhao X, Zhou J, Medina JC, Olson SH.

J Med Chem. 2014 Dec 26;57(24):10499-511. doi: 10.1021/jm501550p. Epub 2014 Dec 4.

PMID:
25384157
8.

Optimization beyond AMG 232: discovery and SAR of sulfonamides on a piperidinone scaffold as potent inhibitors of the MDM2-p53 protein-protein interaction.

Wang Y, Zhu J, Liu JJ, Chen X, Mihalic J, Deignan J, Yu M, Sun D, Kayser F, McGee LR, Lo MC, Chen A, Zhou J, Ye Q, Huang X, Long AM, Yakowec P, Oliner JD, Olson SH, Medina JC.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3782-5. doi: 10.1016/j.bmcl.2014.06.073. Epub 2014 Jul 1.

PMID:
25042256
9.

Novel inhibitors are cytotoxic for myeloma cells with NFkB inducing kinase-dependent activation of NFkB.

Demchenko YN, Brents LA, Li Z, Bergsagel LP, McGee LR, Kuehl MW.

Oncotarget. 2014 Jun 30;5(12):4554-66.

10.

Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.

Li Z, Wang X, Eksterowicz J, Gribble MW Jr, Alba GQ, Ayres M, Carlson TJ, Chen A, Chen X, Cho R, Connors RV, DeGraffenreid M, Deignan JT, Duquette J, Fan P, Fisher B, Fu J, Huard JN, Kaizerman J, Keegan KS, Li C, Li K, Li Y, Liang L, Liu W, Lively SE, Lo MC, Ma J, McMinn DL, Mihalic JT, Modi K, Ngo R, Pattabiraman K, Piper DE, Queva C, Ragains ML, Suchomel J, Thibault S, Walker N, Wang X, Wang Z, Wanska M, Wehn PM, Weidner MF, Zhang AJ, Zhao X, Kamb A, Wickramasinghe D, Dai K, McGee LR, Medina JC.

J Med Chem. 2014 Apr 24;57(8):3430-49. doi: 10.1021/jm500118j. Epub 2014 Apr 2.

PMID:
24641103
11.

Novel inhibitors of the MDM2-p53 interaction featuring hydrogen bond acceptors as carboxylic acid isosteres.

Gonzalez AZ, Li Z, Beck HP, Canon J, Chen A, Chow D, Duquette J, Eksterowicz J, Fox BM, Fu J, Huang X, Houze J, Jin L, Li Y, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, Oliner JD, Osgood T, Rew Y, Saiki AY, Shaffer P, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Olson SH, Sun D, Medina JC.

J Med Chem. 2014 Apr 10;57(7):2963-88. doi: 10.1021/jm401911v. Epub 2014 Mar 27.

PMID:
24601644
12.

Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction.

Gonzalez AZ, Eksterowicz J, Bartberger MD, Beck HP, Canon J, Chen A, Chow D, Duquette J, Fox BM, Fu J, Huang X, Houze JB, Jin L, Li Y, Li Z, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, McMinn DL, Oliner JD, Osgood T, Rew Y, Saiki AY, Shaffer P, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Olson SH, Medina JC, Sun D.

J Med Chem. 2014 Mar 27;57(6):2472-88. doi: 10.1021/jm401767k. Epub 2014 Mar 4.

PMID:
24548297
13.

Preclinical evaluation of AMG 925, a FLT3/CDK4 dual kinase inhibitor for treating acute myeloid leukemia.

Keegan K, Li C, Li Z, Ma J, Ragains M, Coberly S, Hollenback D, Eksterowicz J, Liang L, Weidner M, Huard J, Wang X, Alba G, Orf J, Lo MC, Zhao S, Ngo R, Chen A, Liu L, Carlson T, Quéva C, McGee LR, Medina J, Kamb A, Wickramasinghe D, Dai K.

Mol Cancer Ther. 2014 Apr;13(4):880-9. doi: 10.1158/1535-7163.MCT-13-0858. Epub 2014 Feb 13.

14.

Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.

Sun D, Li Z, Rew Y, Gribble M, Bartberger MD, Beck HP, Canon J, Chen A, Chen X, Chow D, Deignan J, Duquette J, Eksterowicz J, Fisher B, Fox BM, Fu J, Gonzalez AZ, Gonzalez-Lopez De Turiso F, Houze JB, Huang X, Jiang M, Jin L, Kayser F, Liu JJ, Lo MC, Long AM, Lucas B, McGee LR, McIntosh J, Mihalic J, Oliner JD, Osgood T, Peterson ML, Roveto P, Saiki AY, Shaffer P, Toteva M, Wang Y, Wang YC, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Yu M, Zhao X, Zhou J, Zhu J, Olson SH, Medina JC.

J Med Chem. 2014 Feb 27;57(4):1454-72. doi: 10.1021/jm401753e. Epub 2014 Feb 5.

PMID:
24456472
15.

Inhibiting NF-κB-inducing kinase (NIK): discovery, structure-based design, synthesis, structure-activity relationship, and co-crystal structures.

Li K, McGee LR, Fisher B, Sudom A, Liu J, Rubenstein SM, Anwer MK, Cushing TD, Shin Y, Ayres M, Lee F, Eksterowicz J, Faulder P, Waszkowycz B, Plotnikova O, Farrelly E, Xiao SH, Chen G, Wang Z.

Bioorg Med Chem Lett. 2013 Mar 1;23(5):1238-44. doi: 10.1016/j.bmcl.2013.01.012. Epub 2013 Jan 11.

PMID:
23374866
16.

Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity.

Taygerly JP, McGee LR, Rubenstein SM, Houze JB, Cushing TD, Li Y, Motani A, Chen JL, Frankmoelle W, Ye G, Learned MR, Jaen J, Miao S, Timmermans PB, Thoolen M, Kearney P, Flygare J, Beckmann H, Weiszmann J, Lindstrom M, Walker N, Liu J, Biermann D, Wang Z, Hagiwara A, Iida T, Aramaki H, Kitao Y, Shinkai H, Furukawa N, Nishiu J, Nakamura M.

Bioorg Med Chem. 2013 Feb 15;21(4):979-92. doi: 10.1016/j.bmc.2012.11.058. Epub 2012 Dec 10.

PMID:
23294830
17.

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
18.

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
19.

An expeditious synthesis of the MDM2-p53 inhibitor AM-8553.

Lucas BS, Fisher B, McGee LR, Olson SH, Medina JC, Cheung E.

J Am Chem Soc. 2012 Aug 1;134(30):12855-60. doi: 10.1021/ja305123v. Epub 2012 Jul 16.

PMID:
22734631
20.

Imidazo-pyrazine derivatives as potent CXCR3 antagonists.

Du X, Gustin DJ, Chen X, Duquette J, McGee LR, Wang Z, Ebsworth K, Henne K, Lemon B, Ma J, Miao S, Sabalan E, Sullivan TJ, Tonn G, Collins TL, Medina JC.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5200-4. doi: 10.1016/j.bmcl.2009.07.021. Epub 2009 Jul 9.

PMID:
19631529
21.

INT131: a selective modulator of PPAR gamma.

Motani A, Wang Z, Weiszmann J, McGee LR, Lee G, Liu Q, Staunton J, Fang Z, Fuentes H, Lindstrom M, Liu J, Biermann DH, Jaen J, Walker NP, Learned RM, Chen JL, Li Y.

J Mol Biol. 2009 Mar 13;386(5):1301-11.

PMID:
19452630
22.

Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists.

Li AR, Johnson MG, Liu J, Chen X, Du X, Mihalic JT, Deignan J, Gustin DJ, Duquette J, Fu Z, Zhu L, Marcus AP, Bergeron P, McGee LR, Danao J, Lemon B, Carabeo T, Sullivan T, Ma J, Tang L, Tonn G, Collins TL, Medina JC.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):688-93. Epub 2007 Nov 21.

PMID:
18061451
23.

New series of potent, orally bioavailable, non-peptidic cyclic sulfones as HIV-1 protease inhibitors.

Kim CU, McGee LR, Krawczyk SH, Harwood E, Harada Y, Swaminathan S, Bischofberger N, Chen MS, Cherrington JM, Xiong SF, Griffin L, Cundy KC, Lee A, Yu B, Gulnik S, Erickson JW.

J Med Chem. 1996 Aug 30;39(18):3431-4. No abstract available.

PMID:
8784440
24.

Lack of regio- and stereospecificity in oxidation of (+) camphor by Streptomyces griseus enriched in cytochrome P-450soy.

Sariaslani FS, McGee LR, Trower MK, Kitson FG.

Biochem Biophys Res Commun. 1990 Jul 31;170(2):456-61.

PMID:
2116789
25.

Microbial transformation of precocene II: oxidative reactions by Streptomyces griseus.

Sariaslani FS, McGee LR, Ovenall DW.

Appl Environ Microbiol. 1987 Aug;53(8):1780-4.

26.

Light-induced modifications of DNA by gilvocarcin V and its aglycone.

Tse-Dinh YC, McGee LR.

Biochem Biophys Res Commun. 1987 Mar 30;143(3):808-12.

PMID:
3566756
27.

The relative stability of drug prices and pharmacists' fees.

Billups NF, McGee LR.

J Am Pharm Assoc. 1971 Jan;11(1):22-5. No abstract available.

PMID:
5541322

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