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Items: 1 to 20 of 56

1.

Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.

Corte JR, Fang T, Pinto DJ, Orwat MJ, Rendina AR, Luettgen JM, Rossi KA, Wei A, Ramamurthy V, Myers JE Jr, Sheriff S, Narayanan R, Harper TW, Zheng JJ, Li YX, Seiffert DA, Wexler RR, Quan ML.

Bioorg Med Chem. 2016 May 15;24(10):2257-72. doi: 10.1016/j.bmc.2016.03.062. Epub 2016 Apr 1.

PMID:
27073051
2.

Discovery of a Novel 2,6-Disubstituted Glucosamine Series of Potent and Selective Hexokinase 2 Inhibitors.

Lin H, Zeng J, Xie R, Schulz MJ, Tedesco R, Qu J, Erhard KF, Mack JF, Raha K, Rendina AR, Szewczuk LM, Kratz PM, Jurewicz AJ, Cecconie T, Martens S, McDevitt PJ, Martin JD, Chen SB, Jiang Y, Nickels L, Schwartz BJ, Smallwood A, Zhao B, Campobasso N, Qian Y, Briand J, Rominger CM, Oleykowski C, Hardwicke MA, Luengo JI.

ACS Med Chem Lett. 2015 Dec 28;7(3):217-22. doi: 10.1021/acsmedchemlett.5b00214. eCollection 2016 Mar 10.

PMID:
26985301
3.

DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.

Harris PA, King BW, Bandyopadhyay D, Berger SB, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X, Finger JN, Grady LC, Hoffman SJ, Jeong JU, Kang J, Kasparcova V, Lakdawala AS, Lehr R, McNulty DE, Nagilla R, Ouellette MT, Pao CS, Rendina AR, Schaeffer MC, Summerfield JD, Swift BA, Totoritis RD, Ward P, Zhang A, Zhang D, Marquis RW, Bertin J, Gough PJ.

J Med Chem. 2016 Mar 10;59(5):2163-78. doi: 10.1021/acs.jmedchem.5b01898. Epub 2016 Feb 23.

PMID:
26854747
4.

Novel phenylalanine derived diamides as Factor XIa inhibitors.

Smith LM 2nd, Orwat MJ, Hu Z, Han W, Wang C, Rossi KA, Gilligan PJ, Pabbisetty KB, Osuna H, Corte JR, Rendina AR, Luettgen JM, Wong PC, Narayanan R, Harper TW, Bozarth JM, Crain EJ, Wei A, Ramamurthy V, Morin PE, Xin B, Zheng J, Seiffert DA, Quan ML, Lam PY, Wexler RR, Pinto DJ.

Bioorg Med Chem Lett. 2016 Jan 15;26(2):472-8. doi: 10.1016/j.bmcl.2015.11.089. Epub 2015 Nov 26.

PMID:
26704266
5.

New IDH1 mutant inhibitors for treatment of acute myeloid leukemia.

Okoye-Okafor UC, Bartholdy B, Cartier J, Gao EN, Pietrak B, Rendina AR, Rominger C, Quinn C, Smallwood A, Wiggall KJ, Reif AJ, Schmidt SJ, Qi H, Zhao H, Joberty G, Faelth-Savitski M, Bantscheff M, Drewes G, Duraiswami C, Brady P, Groy A, Narayanagari SR, Antony-Debre I, Mitchell K, Wang HR, Kao YR, Christopeit M, Carvajal L, Barreyro L, Paietta E, Makishima H, Will B, Concha N, Adams ND, Schwartz B, McCabe MT, Maciejewski J, Verma A, Steidl U.

Nat Chem Biol. 2015 Nov;11(11):878-86. doi: 10.1038/nchembio.1930. Epub 2015 Oct 5.

PMID:
26436839
6.

In vitro, antithrombotic and bleeding time studies of BMS-654457, a small-molecule, reversible and direct inhibitor of factor XIa.

Wong PC, Quan ML, Watson CA, Crain EJ, Harpel MR, Rendina AR, Luettgen JM, Wexler RR, Schumacher WA, Seiffert DA.

J Thromb Thrombolysis. 2015 Nov;40(4):416-23. doi: 10.1007/s11239-015-1258-7.

PMID:
26249722
7.

Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors.

Priestley ES, Cheney DL, DeLucca I, Wei A, Luettgen JM, Rendina AR, Wong PC, Wexler RR.

J Med Chem. 2015 Aug 13;58(15):6225-36. doi: 10.1021/acs.jmedchem.5b00788. Epub 2015 Jul 28.

PMID:
26151189
8.

Discovery of novel P1 groups for coagulation factor VIIa inhibition using fragment-based screening.

Cheney DL, Bozarth JM, Metzler WJ, Morin PE, Mueller L, Newitt JA, Nirschl AH, Rendina AR, Tamura JK, Wei A, Wen X, Wurtz NR, Seiffert DA, Wexler RR, Priestley ES.

J Med Chem. 2015 Mar 26;58(6):2799-808. doi: 10.1021/jm501982k. Epub 2015 Mar 12.

PMID:
25764119
9.

Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.

Pinto DJ, Smallheer JM, Corte JR, Austin EJ, Wang C, Fang T, Smith LM 2nd, Rossi KA, Rendina AR, Bozarth JM, Zhang G, Wei A, Ramamurthy V, Sheriff S, Myers JE Jr, Morin PE, Luettgen JM, Seiffert DA, Quan ML, Wexler RR.

Bioorg Med Chem Lett. 2015 Apr 1;25(7):1635-42. doi: 10.1016/j.bmcl.2015.01.028. Epub 2015 Feb 4.

PMID:
25728130
10.

Pyridine and pyridinone-based factor XIa inhibitors.

Corte JR, Fang T, Hangeland JJ, Friends TJ, Rendina AR, Luettgen JM, Bozarth JM, Barbera FA, Rossi KA, Wei A, Ramamurthy V, Morin PE, Seiffert DA, Wexler RR, Quan ML.

Bioorg Med Chem Lett. 2015 Feb 15;25(4):925-30. doi: 10.1016/j.bmcl.2014.12.050. Epub 2014 Dec 31.

PMID:
25592713
11.

Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity.

Hangeland JJ, Friends TJ, Rossi KA, Smallheer JM, Wang C, Sun Z, Corte JR, Fang T, Wong PC, Rendina AR, Barbera FA, Bozarth JM, Luettgen JM, Watson CA, Zhang G, Wei A, Ramamurthy V, Morin PE, Bisacchi GS, Subramaniam S, Arunachalam P, Mathur A, Seiffert DA, Wexler RR, Quan ML.

J Med Chem. 2014 Dec 11;57(23):9915-32. doi: 10.1021/jm5010607. Epub 2014 Dec 2.

PMID:
25405503
12.

A human fatty acid synthase inhibitor binds β-ketoacyl reductase in the keto-substrate site.

Hardwicke MA, Rendina AR, Williams SP, Moore ML, Wang L, Krueger JA, Plant RN, Totoritis RD, Zhang G, Briand J, Burkhart WA, Brown KK, Parrish CA.

Nat Chem Biol. 2014 Sep;10(9):774-9. doi: 10.1038/nchembio.1603. Epub 2014 Aug 3.

PMID:
25086508
13.

Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.

Orwat MJ, Qiao JX, He K, Rendina AR, Luettgen JM, Rossi KA, Xin B, Knabb RM, Wexler RR, Lam PY, Pinto DJ.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3341-5. doi: 10.1016/j.bmcl.2014.05.101. Epub 2014 Jun 7.

PMID:
24951330
14.

Design and Synthesis of Phenylpyrrolidine Phenylglycinamides As Highly Potent and Selective TF-FVIIa Inhibitors.

Zhang X, Jiang W, Jacutin-Porte S, Glunz PW, Zou Y, Cheng X, Nirschl AH, Wurtz NR, Luettgen JM, Rendina AR, Luo G, Harper TM, Wei A, Anumula R, Cheney DL, Knabb RM, Wong PC, Wexler RR, Priestley ES.

ACS Med Chem Lett. 2013 Dec 26;5(2):188-92. doi: 10.1021/ml400453z. eCollection 2014 Feb 13.

15.

Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.

Quan ML, Wong PC, Wang C, Woerner F, Smallheer JM, Barbera FA, Bozarth JM, Brown RL, Harpel MR, Luettgen JM, Morin PE, Peterson T, Ramamurthy V, Rendina AR, Rossi KA, Watson CA, Wei A, Zhang G, Seiffert D, Wexler RR.

J Med Chem. 2014 Feb 13;57(3):955-69. doi: 10.1021/jm401670x. Epub 2014 Jan 17.

PMID:
24405333
16.

Outcome of surgically resected thymic carcinoma: a multicenter experience.

Filosso PL, Guerrera F, Rendina AE, Bora G, Ruffini E, Novero D, Ruco L, Vitolo D, Anile M, Ibrahim M, Casadio C, Rena O, Terzi A, Lyberis P, Oliaro A, Venuta F.

Lung Cancer. 2014 Feb;83(2):205-10. doi: 10.1016/j.lungcan.2013.11.015. Epub 2013 Nov 26.

PMID:
24370198
17.

Nonbenzamidine acylsulfonamide tissue factor-factor VIIa inhibitors.

Glunz PW, Zhang X, Zou Y, Delucca I, Nirschl AH, Cheng X, Weigelt CA, Cheney DL, Wei A, Anumula R, Luettgen JM, Rendina AR, Harpel M, Luo G, Knabb R, Wong PC, Wexler RR, Priestley ES.

Bioorg Med Chem Lett. 2013 Sep 15;23(18):5244-8. doi: 10.1016/j.bmcl.2013.06.027. Epub 2013 Jun 21.

PMID:
23845220
18.

Mutant IDH1 enhances the production of 2-hydroxyglutarate due to its kinetic mechanism.

Rendina AR, Pietrak B, Smallwood A, Zhao H, Qi H, Quinn C, Adams ND, Concha N, Duraiswami C, Thrall SH, Sweitzer S, Schwartz B.

Biochemistry. 2013 Jul 2;52(26):4563-77. doi: 10.1021/bi400514k. Epub 2013 Jun 21.

PMID:
23731180
19.

Design and synthesis of bicyclic pyrazinone and pyrimidinone amides as potent TF-FVIIa inhibitors.

Zhang X, Glunz PW, Jiang W, Schmitt A, Newman M, Barbera FA, Bozarth JM, Rendina AR, Wei A, Wen X, Rossi KA, Luettgen JM, Wong PC, Knabb RM, Wexler RR, Scott Priestley E.

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1604-7. doi: 10.1016/j.bmcl.2013.01.094. Epub 2013 Jan 30.

PMID:
23416003
20.

CHROMagar Orientation medium reduces urine culture workload.

Manickam K, Karlowsky JA, Adam H, Lagacé-Wiens PR, Rendina A, Pang P, Murray BL, Alfa MJ.

J Clin Microbiol. 2013 Apr;51(4):1179-83. doi: 10.1128/JCM.02877-12. Epub 2013 Jan 30.

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