Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 1 to 50 of 64

1.

Discovery and Optimization of Quinolinone Derivatives as Potent, Selective, and Orally Bioavailable Mutant Isocitrate Dehydrogenase 1 (mIDH1) Inhibitors.

Lin J, Lu W, Caravella JA, Campbell AM, Diebold RB, Ericsson A, Fritzen E, Gustafson GR, Lancia DR Jr, Shelekhin T, Wang Z, Castro J, Clarke A, Gotur D, Josephine HR, Katz M, Diep H, Kershaw M, Yao L, Kauffman G, Hubbs SE, Luke GP, Toms AV, Wang L, Bair KW, Barr KJ, Dinsmore C, Walker D, Ashwell S.

J Med Chem. 2019 Jul 25;62(14):6575-6596. doi: 10.1021/acs.jmedchem.9b00362. Epub 2019 Jul 8.

PMID:
31199148
2.

MAPK and PI3K signaling: At the crossroads of neural crest development.

Dinsmore CJ, Soriano P.

Dev Biol. 2018 Dec 1;444 Suppl 1:S79-S97. doi: 10.1016/j.ydbio.2018.02.003. Epub 2018 Feb 14. Review.

PMID:
29453943
3.

The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties.

Siu T, Brubaker J, Fuller P, Torres L, Zeng H, Close J, Mampreian DM, Shi F, Liu D, Fradera X, Johnson K, Bays N, Kadic E, He F, Goldenblatt P, Shaffer L, Patel SB, Lesburg CA, Alpert C, Dorosh L, Deshmukh SV, Yu H, Klappenbach J, Elwood F, Dinsmore CJ, Fernandez R, Moy L, Young JR.

J Med Chem. 2017 Dec 14;60(23):9676-9690. doi: 10.1021/acs.jmedchem.7b01135. Epub 2017 Dec 4.

PMID:
29156136
4.

Molecular basis of USP7 inhibition by selective small-molecule inhibitors.

Turnbull AP, Ioannidis S, Krajewski WW, Pinto-Fernandez A, Heride C, Martin ACL, Tonkin LM, Townsend EC, Buker SM, Lancia DR, Caravella JA, Toms AV, Charlton TM, Lahdenranta J, Wilker E, Follows BC, Evans NJ, Stead L, Alli C, Zarayskiy VV, Talbot AC, Buckmelter AJ, Wang M, McKinnon CL, Saab F, McGouran JF, Century H, Gersch M, Pittman MS, Marshall CG, Raynham TM, Simcox M, Stewart LMD, McLoughlin SB, Escobedo JA, Bair KW, Dinsmore CJ, Hammonds TR, Kim S, Urbé S, Clague MJ, Kessler BM, Komander D.

Nature. 2017 Oct 26;550(7677):481-486. doi: 10.1038/nature24451. Epub 2017 Oct 18.

5.

Evaluation of JAK3 Biology in Autoimmune Disease Using a Highly Selective, Irreversible JAK3 Inhibitor.

Elwood F, Witter DJ, Piesvaux J, Kraybill B, Bays N, Alpert C, Goldenblatt P, Qu Y, Ivanovska I, Lee HH, Chiu CS, Tang H, Scott ME, Deshmukh SV, Zielstorff M, Byford A, Chakravarthy K, Dorosh L, Rivkin A, Klappenbach J, Pan BS, Kariv I, Dinsmore C, Slipetz D, Dandliker PJ.

J Pharmacol Exp Ther. 2017 May;361(2):229-244. doi: 10.1124/jpet.116.239723. Epub 2017 Feb 13.

PMID:
28193636
6.

Discovery of MK-1832, a Kv1.5 inhibitor with improved selectivity and pharmacokinetics.

Wolkenberg SE, Nolt MB, Bilodeau MT, Trotter BW, Manley PJ, Kett NR, Nanda KK, Wu Z, Cato MJ, Kane SA, Kiss L, Spencer RH, Wang J, Lynch JJ, Regan CP, Stump GL, Li B, White R, Yeh S, Dinsmore CJ, Lindsley CW, Hartman GD.

Bioorg Med Chem Lett. 2017 Feb 15;27(4):1062-1069. doi: 10.1016/j.bmcl.2016.12.054. Epub 2017 Jan 16.

PMID:
28131713
7.

Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors.

Simov V, Deshmukh SV, Dinsmore CJ, Elwood F, Fernandez RB, Garcia Y, Gibeau C, Gunaydin H, Jung J, Katz JD, Kraybill B, Lapointe B, Patel SB, Siu T, Su H, Young JR.

Bioorg Med Chem Lett. 2016 Apr 1;26(7):1803-8. doi: 10.1016/j.bmcl.2016.02.035. Epub 2016 Feb 19.

PMID:
26927423
8.

Endothelial primary cilia inhibit atherosclerosis.

Dinsmore C, Reiter JF.

EMBO Rep. 2016 Feb;17(2):156-66. doi: 10.15252/embr.201541019. Epub 2016 Jan 14.

9.

The discovery of reverse tricyclic pyridone JAK2 inhibitors. Part 2: lead optimization.

Siu T, Kumarasinghe SE, Altman MD, Katcher M, Northrup A, White C, Rosenstein C, Mathur A, Xu L, Chan G, Bachman E, Bouthillette M, Dinsmore CJ, Marshall CG, Young JR.

Bioorg Med Chem Lett. 2014 Mar 15;24(6):1466-71. doi: 10.1016/j.bmcl.2014.02.011. Epub 2014 Feb 15.

PMID:
24582987
10.

Hedgehog signaling controls T cell killing at the immunological synapse.

de la Roche M, Ritter AT, Angus KL, Dinsmore C, Earnshaw CH, Reiter JF, Griffiths GM.

Science. 2013 Dec 6;342(6163):1247-50. doi: 10.1126/science.1244689.

11.

Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met.

Northrup AB, Katcher MH, Altman MD, Chenard M, Daniels MH, Deshmukh SV, Falcone D, Guerin DJ, Hatch H, Li C, Lu W, Lutterbach B, Allison TJ, Patel SB, Reilly JF, Reutershan M, Rickert KW, Rosenstein C, Soisson SM, Szewczak AA, Walker D, Wilson K, Young JR, Pan BS, Dinsmore CJ.

J Med Chem. 2013 Mar 28;56(6):2294-310. doi: 10.1021/jm301619u. Epub 2013 Mar 18.

PMID:
23379595
12.

Fibrillin-2b regulates endocardial morphogenesis in zebrafish.

Mellman K, Huisken J, Dinsmore C, Hoppe C, Stainier DY.

Dev Biol. 2012 Dec 1;372(1):111-9. doi: 10.1016/j.ydbio.2012.07.015. Epub 2012 Jul 25.

13.

Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.

Lim J, Taoka B, Otte RD, Spencer K, Dinsmore CJ, Altman MD, Chan G, Rosenstein C, Sharma S, Su HP, Szewczak AA, Xu L, Yin H, Zugay-Murphy J, Marshall CG, Young JR.

J Med Chem. 2011 Oct 27;54(20):7334-49. doi: 10.1021/jm200909u. Epub 2011 Sep 26.

PMID:
21942426
14.

Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.

Katz JD, Jewell JP, Guerin DJ, Lim J, Dinsmore CJ, Deshmukh SV, Pan BS, Marshall CG, Lu W, Altman MD, Dahlberg WK, Davis L, Falcone D, Gabarda AE, Hang G, Hatch H, Holmes R, Kunii K, Lumb KJ, Lutterbach B, Mathvink R, Nazef N, Patel SB, Qu X, Reilly JF, Rickert KW, Rosenstein C, Soisson SM, Spencer KB, Szewczak AA, Walker D, Wang W, Young J, Zeng Q.

J Med Chem. 2011 Jun 23;54(12):4092-108. doi: 10.1021/jm200112k. Epub 2011 May 24.

PMID:
21608528
15.

An interstitial duplication at 2q24.3 involving the SCN1A, SCN2A, SCN3A genes associated with infantile epilepsy.

Raymond G, Wohler E, Dinsmore C, Cox J, Johnston M, Batista D, Wang T.

Am J Med Genet A. 2011 Apr;155A(4):920-3. doi: 10.1002/ajmg.a.33929. Epub 2011 Mar 17. No abstract available.

PMID:
21416599
16.

The discovery of tricyclic pyridone JAK2 inhibitors. Part 1: hit to lead.

Siu T, Kozina ES, Jung J, Rosenstein C, Mathur A, Altman MD, Chan G, Xu L, Bachman E, Mo JR, Bouthillette M, Rush T, Dinsmore CJ, Marshall CG, Young JR.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7421-5. doi: 10.1016/j.bmcl.2010.10.031. Epub 2010 Oct 12.

PMID:
21044843
17.

Discovery of triarylethanolamine inhibitors of the Kv1.5 potassium channel.

Beshore DC, Liverton NJ, McIntyre CJ, Claiborne CF, Libby B, Culberson JC, Salata JJ, Regan CP, Lynch JJ, Kiss L, Spencer RH, Kane SA, White RB, Yeh S, Hartman GD, Dinsmore CJ.

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2493-6. doi: 10.1016/j.bmcl.2010.03.005. Epub 2010 Mar 4.

PMID:
20304642
18.

Parallel synthesis of ureas and carbamates from amines and CO2 under mild conditions.

Peterson SL, Stucka SM, Dinsmore CJ.

Org Lett. 2010 Mar 19;12(6):1340-3. doi: 10.1021/ol100259j.

PMID:
20175533
19.

MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.

Pan BS, Chan GK, Chenard M, Chi A, Davis LJ, Deshmukh SV, Gibbs JB, Gil S, Hang G, Hatch H, Jewell JP, Kariv I, Katz JD, Kunii K, Lu W, Lutterbach BA, Paweletz CP, Qu X, Reilly JF, Szewczak AA, Zeng Q, Kohl NE, Dinsmore CJ.

Cancer Res. 2010 Feb 15;70(4):1524-33. doi: 10.1158/0008-5472.CAN-09-2541. Epub 2010 Feb 9.

20.
21.
22.

Design and synthesis of novel isoquinoline-3-nitriles as orally bioavailable Kv1.5 antagonists for the treatment of atrial fibrillation.

Trotter BW, Nanda KK, Kett NR, Regan CP, Lynch JJ, Stump GL, Kiss L, Wang J, Spencer RH, Kane SA, White RB, Zhang R, Anderson KD, Liverton NJ, McIntyre CJ, Beshore DC, Hartman GD, Dinsmore CJ.

J Med Chem. 2006 Nov 30;49(24):6954-7.

PMID:
17125248
23.

Potent antagonists of the Kv1.5 potassium channel: synthesis and evaluation of analogous N,N-diisopropyl-2-(pyridine-3-yl)acetamides.

Nanda KK, Nolt MB, Cato MJ, Kane SA, Kiss L, Spencer RH, Wang J, Lynch JJ, Regan CP, Stump GL, Li B, White R, Yeh S, Bogusky MJ, Bilodeau MT, Dinsmore CJ, Lindsley CW, Hartman GD, Wolkenberg SE, Trotter BW.

Bioorg Med Chem Lett. 2006 Nov 15;16(22):5897-901. Epub 2006 Sep 1.

PMID:
16949818
24.
25.

Biochemical and structural characterization of a novel class of inhibitors of the type 1 insulin-like growth factor and insulin receptor kinases.

Bell IM, Stirdivant SM, Ahern J, Culberson JC, Darke PL, Dinsmore CJ, Drakas RA, Gallicchio SN, Graham SL, Heimbrook DC, Hall DL, Hua J, Kett NR, Kim AS, Kornienko M, Kuo LC, Munshi SK, Quigley AG, Reid JC, Trotter BW, Waxman LH, Williams TM, Zartman CB.

Biochemistry. 2005 Jul 12;44(27):9430-40.

PMID:
15996097
27.

Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.

Dinsmore CJ, Zartman CB, Bergman JM, Abrams MT, Buser CA, Culberson JC, Davide JP, Ellis-Hutchings M, Fernandes C, Graham SL, Hartman GD, Huber HE, Lobell RB, Mosser SD, Robinson RG, Williams TM.

Bioorg Med Chem Lett. 2004 Feb 9;14(3):639-43.

PMID:
14741259
29.
30.

Elastic traction with Essix-based anchorage.

Rinchuse DJ, Rinchuse DJ, Dinsmore C.

J Clin Orthod. 2002 Jan;36(1):46-8. No abstract available.

PMID:
11887643
31.

Evaluation of farnesyl:protein transferase and geranylgeranyl:protein transferase inhibitor combinations in preclinical models.

Lobell RB, Omer CA, Abrams MT, Bhimnathwala HG, Brucker MJ, Buser CA, Davide JP, deSolms SJ, Dinsmore CJ, Ellis-Hutchings MS, Kral AM, Liu D, Lumma WC, Machotka SV, Rands E, Williams TM, Graham SL, Hartman GD, Oliff AI, Heimbrook DC, Kohl NE.

Cancer Res. 2001 Dec 15;61(24):8758-68.

32.

P450 interaction with farnesyl-protein transferase inhibitors metabolic stability, inhibitory potency, and P450 binding spectra in human liver microsomes.

Chiba M, Tang C, Neway WE, Williams TM, Desolms SJ, Dinsmore CJ, Wai JS, Lin JH.

Biochem Pharmacol. 2001 Sep 15;62(6):773-6.

PMID:
11551523
33.

Evaluation of amino acid-based linkers in potent macrocyclic inhibitors of farnesyl-protein transferase.

Beshore DC, Bell IM, Dinsmore CJ, Homnick CF, Culberson JC, Robinson RG, Fernandes C, Walsh ES, Abrams MT, Bhimnathwala HG, Davide JP, Ellis-Hutchings MS, Huber HA, Koblan KS, Buser CA, Kohl NE, Lobell RB, Chen IW, McLoughlin DA, Olah TV, Graham SL, Hartman GD, Williams TM.

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1817-21.

PMID:
11459639
34.

Conformational restriction of flexible ligands guided by the transferred noe experiment: potent macrocyclic inhibitors of farnesyltransferase.

Dinsmore CJ, Bogusky MJ, Culberson JC, Bergman JM, Homnick CF, Zartman CB, Mosser SD, Schaber MD, Robinson RG, Koblan KS, Huber HE, Graham SL, Hartman GD, Huff JR, Williams TM.

J Am Chem Soc. 2001 Mar 7;123(9):2107-8. No abstract available.

PMID:
11456854
35.

Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.

Bergman JM, Abrams MT, Davide JP, Greenberg IB, Robinson RG, Buser CA, Huber HE, Koblan KS, Kohl NE, Lobell RB, Graham SL, Hartman GD, Williams TM, Dinsmore CJ.

Bioorg Med Chem Lett. 2001 Jun 4;11(11):1411-5.

PMID:
11378366
36.

Student responses to the gross anatomy laboratory in a medical curriculum.

Dinsmore CE, Daugherty S, Zeitz HJ.

Clin Anat. 2001 May;14(3):231-6.

PMID:
11301472
37.

2-Arylindole-3-acetamides: FPP-competitive inhibitors of farnesyl protein transferase.

Trotter BW, Quigley AG, Lumma WC, Sisko JT, Walsh ES, Hamann CS, Robinson RG, Bhimnathwala H, Kolodin DG, Zheng W, Buser CA, Huber HE, Lobell RB, Kohl NE, Williams TM, Graham SL, Dinsmore CJ.

Bioorg Med Chem Lett. 2001 Apr 9;11(7):865-9.

PMID:
11294379
38.

Anions modulate the potency of geranylgeranyl-protein transferase I inhibitors.

Huber HE, Robinson RG, Watkins A, Nahas DD, Abrams MT, Buser CA, Lobell RB, Patrick D, Anthony NJ, Dinsmore CJ, Graham SL, Hartman GD, Lumma WC, Williams TM, Heimbrook DC.

J Biol Chem. 2001 Jul 6;276(27):24457-65. Epub 2001 Mar 26.

39.

3,8-Diazabicyclo[3.2.1]octan-2-one peptide mimetics: synthesis of a conformationally restricted inhibitor of farnesyltransferase.

Dinsmore CJ, Bergman JM, Bogusky MJ, Culberson JC, Hamilton KA, Graham SL.

Org Lett. 2001 Mar 22;3(6):865-8.

PMID:
11263902
40.

Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase.

Dinsmore CJ, Bergman JM, Wei DD, Zartman CB, Davide JP, Greenberg IB, Liu D, O'Neill TJ, Gibbs JB, Koblan KS, Kohl NE, Lobell RB, Chen IW, McLoughlin DA, Olah TV, Graham SL, Hartman GD, Williams TM.

Bioorg Med Chem Lett. 2001 Feb 26;11(4):537-40.

PMID:
11229765
41.

High-performance liquid chromatography/mass spectrometry characterization of Ki4B-Ras in PSN-1 cells treated with the prenyltransferase inhibitor L-778,123.

Buser CA, Dinsmore CJ, Fernandes C, Greenberg I, Hamilton K, Mosser SD, Walsh ES, Williams TM, Koblan KS.

Anal Biochem. 2001 Mar 1;290(1):126-37.

PMID:
11180946
42.

Synthesis of conformationally constrained 5,6,7, 8-Tetrahydroimidazo[1,5-a]pyridine inhibitors of farnesyltransferase.

Dinsmore CJ, Zartman CB, Baginsky WF, O'Neill TJ, Koblan KS, Chen IW, McLoughlin DA, Olah TV, Huff JR.

Org Lett. 2000 Nov 2;2(22):3473-6.

PMID:
11082012
43.

Imidazole-containing diarylether and diarylsulfone inhibitors of farnesyl-protein transferase.

Dinsmore CJ, Williams TM, O'Neill TJ, Liu D, Rands E, Culberson JC, Lobell RB, Koblan KS, Kohl NE, Gibbs JB, Oliff AI, Graham SL, Hartman GD.

Bioorg Med Chem Lett. 1999 Dec 6;9(23):3301-6.

PMID:
10612589
44.

N-arylpiperazinone inhibitors of farnesyltransferase: discovery and biological activity.

Williams TM, Bergman JM, Brashear K, Breslin MJ, Dinsmore CJ, Hutchinson JH, MacTough SC, Stump CA, Wei DD, Zartman CB, Bogusky MJ, Culberson JC, Buser-Doepner C, Davide J, Greenberg IB, Hamilton KA, Koblan KS, Kohl NE, Liu D, Lobell RB, Mosser SD, O'Neill TJ, Rands E, Schaber MD, Huff JR, et al.

J Med Chem. 1999 Sep 23;42(19):3779-84. No abstract available.

PMID:
10508426
45.

Non-thiol 3-aminomethylbenzamide inhibitors of farnesyl-protein transferase.

Ciccarone TM, MacTough SC, Williams TM, Dinsmore CJ, O'Neill TJ, Shah D, Culberson JC, Koblan KS, Kohl NE, Gibbs JB, Oliff AI, Graham SL, Hartman GD.

Bioorg Med Chem Lett. 1999 Jul 19;9(14):1991-6.

PMID:
10450968
46.

Teaching and learning gross anatomy: dissection, prosection, or "both of the above?".

Dinsmore CE, Daugherty S, Zeitz HJ.

Clin Anat. 1999;12(2):110-4. Review. No abstract available.

PMID:
10089036
47.
48.

Nonconventional Stereochemical Issues in the Design of the Synthesis of the Vancomycin Antibiotics: Challenges Imposed by Axial and Nonplanar Chiral Elements in the Heptapeptide Aglycons.

Evans DA, Dinsmore CJ, Watson PS, Wood MR, Richardson TI, Trotter BW, Katz JL.

Angew Chem Int Ed Engl. 1998 Oct 16;37(19):2704-2708. doi: 10.1002/(SICI)1521-3773(19981016)37:19<2704::AID-ANIE2704>3.0.CO;2-1.

PMID:
29711602
49.

In memoriam: Richard J. Goss, 1925-1996.

Dinsmore CE, Aronson SM.

J Exp Zool. 1997 Mar 1;277(4):353-5. No abstract available.

PMID:
9097463
50.

Farnesyl: proteintransferase inhibitors as agents to inhibit tumor growth.

Omer CA, Anthony NJ, Buser-Doepner CA, Burkhardt AL, deSolms SJ, Dinsmore CJ, Gibbs JB, Hartman GD, Koblan KS, Lobell RB, Oliff A, Williams TM, Kohl NE.

Biofactors. 1997;6(3):359-66. Review.

PMID:
9288406

Supplemental Content

Loading ...
Support Center