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Items: 9

1.

Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer.

Gross MI, Demo SD, Dennison JB, Chen L, Chernov-Rogan T, Goyal B, Janes JR, Laidig GJ, Lewis ER, Li J, Mackinnon AL, Parlati F, Rodriguez ML, Shwonek PJ, Sjogren EB, Stanton TF, Wang T, Yang J, Zhao F, Bennett MK.

Mol Cancer Ther. 2014 Apr;13(4):890-901. doi: 10.1158/1535-7163.MCT-13-0870. Epub 2014 Feb 12.

2.

Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase.

Goldstein DM, Soth M, Gabriel T, Dewdney N, Kuglstatter A, Arzeno H, Chen J, Bingenheimer W, Dalrymple SA, Dunn J, Farrell R, Frauchiger S, La Fargue J, Ghate M, Graves B, Hill RJ, Li F, Litman R, Loe B, McIntosh J, McWeeney D, Papp E, Park J, Reese HF, Roberts RT, Rotstein D, San Pablo B, Sarma K, Stahl M, Sung ML, Suttman RT, Sjogren EB, Tan Y, Trejo A, Welch M, Weller P, Wong BR, Zecic H.

J Med Chem. 2011 Apr 14;54(7):2255-65. doi: 10.1021/jm101423y. Epub 2011 Mar 4.

PMID:
21375264
3.

A novel series of IKKβ inhibitors part I: Initial SAR studies of a HTS hit.

Cushing TD, Baichwal V, Berry K, Billedeau R, Bordunov V, Broka C, Cardozo M, Cheng P, Clark D, Dalrymple S, DeGraffenreid M, Gill A, Hao X, Hawley RC, He X, Jaen JC, Labadie SS, Labelle M, Lehel C, Lu PP, McIntosh J, Miao S, Parast C, Shin Y, Sjogren EB, Smith ML, Talamas FX, Tonn G, Walker KM, Walker NP, Wesche H, Whitehead C, Wright M, Browner MF.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):417-22. doi: 10.1016/j.bmcl.2010.10.126. Epub 2010 Oct 29.

PMID:
21074993
4.

A novel series of IKKβ inhibitors part II: description of a potent and pharmacologically active series of analogs.

Cushing TD, Baichwal V, Berry K, Billedeau R, Bordunov V, Broka C, Browner MF, Cardozo M, Cheng P, Clark D, Dalrymple S, DeGraffenreid M, Gill A, Hao X, Hawley RC, He X, Labadie SS, Labelle M, Lehel C, Lu PP, McIntosh J, Miao S, Parast C, Shin Y, Sjogren EB, Smith ML, Talamas FX, Tonn G, Walker KM, Walker NP, Wesche H, Whitehead C, Wright M, Jaen JC.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):423-6. doi: 10.1016/j.bmcl.2010.10.125. Epub 2010 Oct 29.

PMID:
21074992
5.

Discovery of S-[5-amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]-[3-(2,3-dihydroxypropoxy)phenyl]methanone (RO3201195), an orally bioavailable and highly selective inhibitor of p38 MAP kinase.

Goldstein DM, Alfredson T, Bertrand J, Browner MF, Clifford K, Dalrymple SA, Dunn J, Freire-Moar J, Harris S, Labadie SS, La Fargue J, Lapierre JM, Larrabee S, Li F, Papp E, McWeeney D, Ramesha C, Roberts R, Rotstein D, San Pablo B, Sjogren EB, So OY, Talamas FX, Tao W, Trejo A, Villasenor A, Welch M, Welch T, Weller P, Whiteley PE, Young K, Zipfel S.

J Med Chem. 2006 Mar 9;49(5):1562-75.

PMID:
16509574
6.

N-arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective alpha 1-adrenoceptor antagonists.

Elworthy TR, Ford AP, Bantle GW, Morgans DJ Jr, Ozer RS, Palmer WS, Repke DB, Romero M, Sandoval L, Sjogren EB, Talamás FX, Vazquez A, Wu H, Arredondo NF, Blue DR Jr, DeSousa A, Gross LM, Kava MS, Lesnick JD, Vimont RL, Williams TJ, Zhu QM, Pfister JR, Clarke DE.

J Med Chem. 1997 Aug 15;40(17):2674-87.

PMID:
9276013
7.

Structure-activity relationships for inhibition of inosine monophosphate dehydrogenase by nuclear variants of mycophenolic acid.

Nelson PH, Carr SF, Devens BH, Eugui EM, Franco F, Gonzalez C, Hawley RC, Loughhead DG, Milan DJ, Papp E, Patterson JW, Rouhafza S, Sjogren EB, Smith DB, Stephenson RA, Talamas FX, Waltos AM, Weikert RJ, Wu JC.

J Med Chem. 1996 Oct 11;39(21):4181-96.

PMID:
8863796
8.

Synthesis and biological activity of a series of diaryl-substituted alpha-cyano-beta-hydroxypropenamides, a new class of anthelmintic agents.

Sjogren EB, Rider MA, Nelson PH, Bingham S Jr, Poulton AL, Emanuel MA, Komuniecki R.

J Med Chem. 1991 Nov;34(11):3295-301.

PMID:
1956049
9.

Antitrichomonal activity of mesoionic thiazolo[3,2-a]pyridines.

Walker KA, Sjogren EB, Matthews TR.

J Med Chem. 1985 Nov;28(11):1673-9.

PMID:
4067993

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