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Items: 49

1.

Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage.

Hart AC, Abell L, Guo J, Mertzman ME, Padmanabha R, Macor JE, Chaudhry C, Lu H, O'Malley K, Shaw PJ, Weigelt C, Pokross M, Kish K, Kim KS, Cornelius L, Douglas AE, Calambur D, Zhang P, Carpenter B, Pitts WJ.

ACS Med Chem Lett. 2019 May 6;11(3):266-271. doi: 10.1021/acsmedchemlett.9b00065. eCollection 2020 Mar 12.

PMID:
32184955
2.

Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.

Wrobleski ST, Moslin R, Lin S, Zhang Y, Spergel S, Kempson J, Tokarski JS, Strnad J, Zupa-Fernandez A, Cheng L, Shuster D, Gillooly K, Yang X, Heimrich E, McIntyre KW, Chaudhry C, Khan J, Ruzanov M, Tredup J, Mulligan D, Xie D, Sun H, Huang C, D'Arienzo C, Aranibar N, Chiney M, Chimalakonda A, Pitts WJ, Lombardo L, Carter PH, Burke JR, Weinstein DS.

J Med Chem. 2019 Oct 24;62(20):8973-8995. doi: 10.1021/acs.jmedchem.9b00444. Epub 2019 Jul 18.

PMID:
31318208
3.

Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.

Spergel SH, Mertzman ME, Kempson J, Guo J, Stachura S, Haque L, Lippy JS, Zhang RF, Galella M, Pitt S, Shen G, Fura A, Gillooly K, McIntyre KW, Tang V, Tokarski J, Sack JS, Khan J, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, Schieven GL, Wrobleski ST, Pitts WJ.

ACS Med Chem Lett. 2019 Feb 13;10(3):306-311. doi: 10.1021/acsmedchemlett.8b00508. eCollection 2019 Mar 14.

4.

Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors.

Bhide RS, Keon A, Weigelt C, Sack JS, Schmidt RJ, Lin S, Xiao HY, Spergel SH, Kempson J, Pitts WJ, Carman J, Poss MA.

Bioorg Med Chem Lett. 2017 Nov 1;27(21):4908-4913. doi: 10.1016/j.bmcl.2017.09.029. Epub 2017 Sep 18.

PMID:
28947151
5.

Discovery of highly potent, selective, covalent inhibitors of JAK3.

Kempson J, Ovalle D, Guo J, Wrobleski ST, Lin S, Spergel SH, Duan JJ, Jiang B, Lu Z, Das J, Yang BV, Hynes J Jr, Wu H, Tokarski J, Sack JS, Khan J, Schieven G, Blatt Y, Chaudhry C, Salter-Cid LM, Fura A, Barrish JC, Carter PH, Pitts WJ.

Bioorg Med Chem Lett. 2017 Oct 15;27(20):4622-4625. doi: 10.1016/j.bmcl.2017.09.023. Epub 2017 Sep 11.

PMID:
28927786
6.

Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.

Hynes J Jr, Wu H, Kempson J, Duan JJ, Lu Z, Jiang B, Stachura S, Tokarski JS, Sack JS, Khan JA, Lippy JS, Zhang RF, Pitt S, Shen G, Gillooly K, McIntyre K, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, Fura A, Schieven GL, Pitts WJ, Wrobleski ST.

Bioorg Med Chem Lett. 2017 Jul 15;27(14):3101-3106. doi: 10.1016/j.bmcl.2017.05.043. Epub 2017 May 15.

PMID:
28539220
7.

Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1).

Gilmore JL, Sheppeck JE 2nd, Watterson SH, Haque L, Mukhopadhyay P, Tebben AJ, Galella MA, Shen DR, Yarde M, Cvijic ME, Borowski V, Gillooly K, Taylor T, McIntyre KW, Warrack B, Levesque PC, Li JP, Cornelius G, D'Arienzo C, Marino A, Balimane P, Salter-Cid L, Barrish JC, Pitts WJ, Carter PH, Xie J, Dyckman AJ.

J Med Chem. 2016 Jul 14;59(13):6248-64. doi: 10.1021/acs.jmedchem.6b00373. Epub 2016 Jul 1.

PMID:
27309907
8.

Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1).

Guo J, Watterson SH, Spergel SH, Kempson J, Langevine CM, Shen DR, Yarde M, Cvijic ME, Banas D, Liu R, Suchard SJ, Gillooly K, Taylor T, Rex-Rabe S, Shuster DJ, McIntyre KW, Cornelius G, D'Arienzo C, Marino A, Balimane P, Salter-Cid L, McKinnon M, Barrish JC, Carter PH, Pitts WJ, Xie J, Dyckman AJ.

Bioorg Med Chem Lett. 2016 May 15;26(10):2470-2474. doi: 10.1016/j.bmcl.2016.03.105. Epub 2016 Apr 1.

PMID:
27055941
9.

Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.

Watterson SH, Guo J, Spergel SH, Langevine CM, Moquin RV, Shen DR, Yarde M, Cvijic ME, Banas D, Liu R, Suchard SJ, Gillooly K, Taylor T, Rex-Rabe S, Shuster DJ, McIntyre KW, Cornelius G, D'Arienzo C, Marino A, Balimane P, Warrack B, Salter-Cid L, McKinnon M, Barrish JC, Carter PH, Pitts WJ, Xie J, Dyckman AJ.

J Med Chem. 2016 Mar 24;59(6):2820-40. doi: 10.1021/acs.jmedchem.6b00089. Epub 2016 Mar 10.

PMID:
26924461
10.

Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.

Hart AC, Schroeder GM, Wan H, Grebinski J, Inghrim J, Kempson J, Guo J, Pitts WJ, Tokarski JS, Sack JS, Khan JA, Lippy J, Lorenzi MV, You D, McDevitt T, Vuppugalla R, Zhang Y, Lombardo LJ, Trainor GL, Purandare AV.

ACS Med Chem Lett. 2015 Jul 10;6(8):845-9. doi: 10.1021/acsmedchemlett.5b00225. eCollection 2015 Aug 13.

11.

Organic chemistry. Practical olefin hydroamination with nitroarenes.

Gui J, Pan CM, Jin Y, Qin T, Lo JC, Lee BJ, Spergel SH, Mertzman ME, Pitts WJ, La Cruz TE, Schmidt MA, Darvatkar N, Natarajan SR, Baran PS.

Science. 2015 May 22;348(6237):886-91. doi: 10.1126/science.aab0245. Epub 2015 May 21.

12.

Tyrosine Kinase 2-mediated Signal Transduction in T Lymphocytes Is Blocked by Pharmacological Stabilization of Its Pseudokinase Domain.

Tokarski JS, Zupa-Fernandez A, Tredup JA, Pike K, Chang C, Xie D, Cheng L, Pedicord D, Muckelbauer J, Johnson SR, Wu S, Edavettal SC, Hong Y, Witmer MR, Elkin LL, Blat Y, Pitts WJ, Weinstein DS, Burke JR.

J Biol Chem. 2015 Apr 24;290(17):11061-74. doi: 10.1074/jbc.M114.619502. Epub 2015 Mar 11.

13.

Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.

Duan JJ, Lu Z, Jiang B, Yang BV, Doweyko LM, Nirschl DS, Haque LE, Lin S, Brown G, Hynes J Jr, Tokarski JS, Sack JS, Khan J, Lippy JS, Zhang RF, Pitt S, Shen G, Pitts WJ, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, McKinnon M, Fura A, Schieven GL, Wrobleski ST.

Bioorg Med Chem Lett. 2014 Dec 15;24(24):5721-5726. doi: 10.1016/j.bmcl.2014.10.061. Epub 2014 Oct 24.

PMID:
25453808
14.

Organic chemistry: Toolkit of reagents to aid drug discovery.

Pitts WJ.

Nature. 2012 Dec 6;492(7427):45-6. doi: 10.1038/nature11760. Epub 2012 Nov 28. No abstract available.

PMID:
23201687
15.

Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).

Watterson SH, Langevine CM, Van Kirk K, Kempson J, Guo J, Spergel SH, Das J, Moquin RV, Dyckman AJ, Nirschl D, Gregor K, Pattoli MA, Yang X, McIntyre KW, Yang G, Galella MA, Booth-Lute H, Chen L, Yang Z, Wang-Iverson D, McKinnon M, Dodd JH, Barrish JC, Burke JR, Pitts WJ.

Bioorg Med Chem Lett. 2011 Dec 1;21(23):7006-12. doi: 10.1016/j.bmcl.2011.09.111. Epub 2011 Oct 5.

PMID:
22018461
16.

Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.

Dyckman AJ, Langevine CM, Quesnelle C, Kempson J, Guo J, Gill P, Spergel SH, Watterson SH, Li T, Nirschl DS, Gillooly KM, Pattoli MA, McIntyre KW, Chen L, McKinnon M, Dodd JH, Barrish JC, Burke JR, Pitts WJ.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):383-6. doi: 10.1016/j.bmcl.2010.10.133. Epub 2010 Oct 31.

PMID:
21087862
17.

Periodic, partial inhibition of IkappaB Kinase beta-mediated signaling yields therapeutic benefit in preclinical models of rheumatoid arthritis.

Gillooly KM, Pattoli MA, Taylor TL, Chen L, Cheng L, Gregor KR, Whitney GS, Susulic V, Watterson SH, Kempson J, Pitts WJ, Booth-Lute H, Yang G, Davies P, Kukral DW, Strnad J, McIntyre KW, Darienzo CJ, Salter-Cid L, Yang Z, Wang-Iverson DB, Burke JR.

J Pharmacol Exp Ther. 2009 Nov;331(2):349-60. doi: 10.1124/jpet.109.156018. Epub 2009 Aug 3.

PMID:
19652024
18.

Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase.

Kempson J, Guo J, Das J, Moquin RV, Spergel SH, Watterson SH, Langevine CM, Dyckman AJ, Pattoli M, Burke JR, Yang X, Gillooly KM, McIntyre KW, Chen L, Dodd JH, McKinnon M, Barrish JC, Pitts WJ.

Bioorg Med Chem Lett. 2009 May 15;19(10):2646-9. doi: 10.1016/j.bmcl.2009.03.159. Epub 2009 Apr 5.

PMID:
19376699
19.

Identification of potent pyrimidine inhibitors of phosphodiesterase 7 (PDE7) and their ability to inhibit T cell proliferation.

Guo J, Watson A, Kempson J, Carlsen M, Barbosa J, Stebbins K, Lee D, Dodd J, Nadler SG, McKinnon M, Barrish J, Pitts WJ.

Bioorg Med Chem Lett. 2009 Apr 1;19(7):1935-8. doi: 10.1016/j.bmcl.2009.02.060. Epub 2009 Feb 21.

PMID:
19272774
20.

Novel tricyclic inhibitors of IkappaB kinase.

Kempson J, Spergel SH, Guo J, Quesnelle C, Gill P, Belanger D, Dyckman AJ, Li T, Watterson SH, Langevine CM, Das J, Moquin RV, Furch JA, Marinier A, Dodier M, Martel A, Nirschl D, Van Kirk K, Burke JR, Pattoli MA, Gillooly K, McIntyre KW, Chen L, Yang Z, Marathe PH, Wang-Iverson D, Dodd JH, McKinnon M, Barrish JC, Pitts WJ.

J Med Chem. 2009 Apr 9;52(7):1994-2005. doi: 10.1021/jm8015816.

PMID:
19267461
21.

Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships.

Kempson J, Pitts WJ, Barbosa J, Guo J, Omotoso O, Watson A, Stebbins K, Starling GC, Dodd JH, Barrish JC, Felix R, Fischer K.

Bioorg Med Chem Lett. 2005 Apr 1;15(7):1829-33.

PMID:
15780616
22.

Identification of purine inhibitors of phosphodiesterase 7 (PDE7).

Pitts WJ, Vaccaro W, Huynh T, Leftheris K, Roberge JY, Barbosa J, Guo J, Brown B, Watson A, Donaldson K, Starling GC, Kiener PA, Poss MA, Dodd JH, Barrish JC.

Bioorg Med Chem Lett. 2004 Jun 7;14(11):2955-8.

PMID:
15125967
23.

Phosphodiesterase 7A-deficient mice have functional T cells.

Yang G, McIntyre KW, Townsend RM, Shen HH, Pitts WJ, Dodd JH, Nadler SG, McKinnon M, Watson AJ.

J Immunol. 2003 Dec 15;171(12):6414-20.

24.

Inhibitors of inosine monophosphate dehydrogenase: SARs about the N-[3-Methoxy-4-(5-oxazolyl)phenyl moiety.

Iwanowicz EJ, Watterson SH, Guo J, Pitts WJ, Murali Dhar TG, Shen Z, Chen P, Gu HH, Fleener CA, Rouleau KA, Cheney DL, Townsend RM, Hollenbaugh DL.

Bioorg Med Chem Lett. 2003 Jun 16;13(12):2059-63.

PMID:
12781195
25.

Identification of novel and potent isoquinoline aminooxazole-based IMPDH inhibitors.

Chen P, Norris D, Haslow KD, Murali Dhar TG, Pitts WJ, Watterson SH, Cheney DL, Bassolino DA, Fleener CA, Rouleau KA, Hollenbaugh DL, Townsend RM, Barrish JC, Iwanowicz EJ.

Bioorg Med Chem Lett. 2003 Apr 7;13(7):1345-8.

PMID:
12657279
26.

Quinolone-based IMPDH inhibitors: introduction of basic residues on ring D and SAR of the corresponding mono, di and benzofused analogues.

Dhar TG, Watterson SH, Chen P, Shen Z, Gu HH, Norris D, Carlsen M, Haslow KD, Pitts WJ, Guo J, Chorba J, Fleener CA, Rouleau KA, Townsend R, Hollenbaugh D, Iwanowicz EJ.

Bioorg Med Chem Lett. 2003 Feb 10;13(3):547-51.

PMID:
12565969
27.

Novel inhibitors of IMPDH: a highly potent and selective quinolone-based series.

Watterson SH, Carlsen M, Dhar TG, Shen Z, Pitts WJ, Guo J, Gu HH, Norris D, Chorba J, Chen P, Cheney D, Witmer M, Fleener CA, Rouleau K, Townsend R, Hollenbaugh DL, Iwanowicz EJ.

Bioorg Med Chem Lett. 2003 Feb 10;13(3):543-6.

PMID:
12565968
28.

A survey of cyclic replacements for the central diamide moiety of inhibitors of inosine monophosphate dehydrogenase.

Dhar TG, Liu C, Pitts WJ, Guo J, Watterson SH, Gu H, Fleener CA, Rouleau K, Sherbina NZ, Barrish JC, Hollenbaugh D, Iwanowicz EJ.

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3125-8.

PMID:
12372516
29.

Novel amide-based inhibitors of inosine 5'-monophosphate dehydrogenase.

Watterson SH, Liu C, Dhar TG, Gu HH, Pitts WJ, Barrish JC, Fleener CA, Rouleau K, Sherbina NZ, Hollenbaugh DL, Iwanowicz EJ.

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2879-82.

PMID:
12270168
30.

Rapid synthesis of triazine inhibitors of inosine monophosphate dehydrogenase.

Pitts WJ, Guo J, Dhar TG, Shen Z, Gu HH, Watterson SH, Bednarz MS, Chen BC, Barrish JC, Bassolino D, Cheney D, Fleener CA, Rouleau KA, Hollenbaugh DL, Iwanowicz EJ.

Bioorg Med Chem Lett. 2002 Aug 19;12(16):2137-40.

PMID:
12127522
31.

A modified approach to 2-(N-aryl)-1,3-oxazoles: application to the synthesis of the IMPDH inhibitor BMS-337197 and analogues.

Dhar TG, Guo J, Shen Z, Pitts WJ, Gu HH, Chen BC, Zhao R, Bednarz MS, Iwanowicz EJ.

Org Lett. 2002 Jun 13;4(12):2091-3.

PMID:
12049525
32.

Discovery of N-[2-[2-[[3-methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4- morpholineacetamide as a novel and potent inhibitor of inosine monophosphate dehydrogenase with excellent in vivo activity.

Dhar TG, Shen Z, Guo J, Liu C, Watterson SH, Gu HH, Pitts WJ, Fleener CA, Rouleau KA, Sherbina NZ, McIntyre KW, Shuster DJ, Witmer MR, Tredup JA, Chen BC, Zhao R, Bednarz MS, Cheney DL, MacMaster JF, Miller LM, Berry KK, Harper TW, Barrish JC, Hollenbaugh DL, Iwanowicz EJ.

J Med Chem. 2002 May 23;45(11):2127-30. Erratum in: J Med Chem2002 Nov 7;45(23):5188.

PMID:
12014950
33.

Novel diamide-based inhibitors of IMPDH.

Gu HH, Iwanowicz EJ, Guo J, Watterson SH, Shen Z, Pitts WJ, Dhar TG, Fleener CA, Rouleau K, Sherbina NZ, Witmer M, Tredup J, Hollenbaugh D.

Bioorg Med Chem Lett. 2002 May 6;12(9):1323-6.

PMID:
11965381
34.

Retinoic acid and vitamin E modulate expression and release of CD178 in carcinoma cells: consequences for induction of apoptosis in CD95-sensitive cells.

Salih HR, Starling GC, Knauff M, Llewellyn MB, Davis PM, Pitts WJ, Aruffo A, Kiener PA.

Exp Cell Res. 2001 Nov 1;270(2):248-58.

PMID:
11640888
35.

Isoxazolines as potent antagonists of the integrin alpha(v)beta(3).

Pitts WJ, Wityak J, Smallheer JM, Tobin AE, Jetter JW, Buynitsky JS, Harlow PP, Solomon KA, Corjay MH, Mousa SA, Wexler RR, Jadhav PK.

J Med Chem. 2000 Jan 13;43(1):27-40.

PMID:
10633036
36.

Rapid synthesis of RGD mimetics with isoxazoline scaffolds on solid phase: identification of alphavbeta3 antagonists lead compounds.

Rockwell AL, Rafalski M, Pitts WJ, Batt DG, Petraitis JJ, DeGrado WF, Mousa S, Jadhav PK.

Bioorg Med Chem Lett. 1999 Apr 5;9(7):937-42.

PMID:
10230615
37.

Terphenyl cyclooxygenase-2 (COX-2) inhibitors: optimization of the central ring and o-biphenyl analogs.

Pinto DJ, Batt DG, Pitts WJ, Petraitis JJ, Orwat MJ, Wang S, Jetter JW, Sherk SR, Houghton GC, Copeland RA, Covington MB, Trzaskos JM, Magolda RL.

Bioorg Med Chem Lett. 1999 Apr 5;9(7):919-24.

PMID:
10230611
38.

MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.

Duncia JV, Santella JB 3rd, Higley CA, Pitts WJ, Wityak J, Frietze WE, Rankin FW, Sun JH, Earl RA, Tabaka AC, Teleha CA, Blom KF, Favata MF, Manos EJ, Daulerio AJ, Stradley DA, Horiuchi K, Copeland RA, Scherle PA, Trzaskos JM, Magolda RL, Trainor GL, Wexler RR, Hobbs FW, Olson RE.

Bioorg Med Chem Lett. 1998 Oct 20;8(20):2839-44.

PMID:
9873633
39.

Structure-activity relationships (SAR) of some tetracyclic heterocycles related to the immunosuppressive agent Brequinar Sodium.

Pitts WJ, Jetter JW, Pinto DJ, Orwat MJ, Batt DG, Sherk SR, Petraitis JJ, Jacobson IC, Copeland RA, Dowling RL, Jaffee BD, Gardner TL, Jones EA, Magolda RL.

Bioorg Med Chem Lett. 1998 Feb 3;8(3):307-12.

PMID:
9871675
40.

Identification of a novel inhibitor of mitogen-activated protein kinase kinase.

Favata MF, Horiuchi KY, Manos EJ, Daulerio AJ, Stradley DA, Feeser WS, Van Dyk DE, Pitts WJ, Earl RA, Hobbs F, Copeland RA, Magolda RL, Scherle PA, Trzaskos JM.

J Biol Chem. 1998 Jul 17;273(29):18623-32.

41.

Sodium economy in white-tailed deer (Odocoileus virginianus).

Hellgren EC, Pitts WJ.

Physiol Zool. 1997 Sep-Oct;70(5):547-55.

PMID:
9279921
42.

The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase.

Davis JP, Cain GA, Pitts WJ, Magolda RL, Copeland RA.

Biochemistry. 1996 Jan 30;35(4):1270-3.

PMID:
8573583
43.

Sebaceous adenocarcinoma.

Wilborn WH, Pitts WJ, Montes LF.

J Cutan Pathol. 1981 Jun;8(3):266-70. No abstract available.

PMID:
7309940
44.

Absorption, excretion, and retention of orally administered zinc-65 in various tissues of zinc-deficient and normal goats and calves.

Miller WJ, Blackmon DM, Gentry RP, Pitts WJ, Powell GW.

J Nutr. 1967 May;92(1):71-8. No abstract available.

PMID:
6028306
45.

Plastic surgery in the management of paraplegics.

Pitts WJ.

Ala J Med Sci. 1967 Apr;4(2):140-2. No abstract available.

PMID:
6036703
46.

Effect of zinc deficiency and restricted feeding from two to five months of age on reproduction in Holstein bulls.

Pitts WJ, Miller WJ, Fosgate OT, Morton JD, Clifton CM.

J Dairy Sci. 1966 Aug;49(8):995-1000. No abstract available.

47.
48.

Factors affecting zinc content bovine hair.

Miller WJ, Powell GW, Pitts WJ, Perkins HF.

J Dairy Sci. 1965 Aug;48(8):1091-5. No abstract available.

PMID:
5837882
49.

EFFECT OF ZINC DEFICIENCY AND RESTRICTED FEEDING ON WOUND HEALING IN THE BOVINE.

MILLER WJ, MORTON JD, PITTS WJ, CLIFTON CM.

Proc Soc Exp Biol Med. 1965 Feb;118:427-30. No abstract available.

PMID:
14268643

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