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Items: 17

1.

A highly selective, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor has potent activity in vitro and in vivo.

LaMontagne KR, Butler J, Borowski VB, Fuentes-Pesquera AR, Blevitt JM, Huang S, Li R, Connolly PJ, Greenberger LM.

Angiogenesis. 2009;12(3):287-96. doi: 10.1007/s10456-009-9151-7. Epub 2009 Jun 21.

PMID:
19544081
2.

Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors.

Lin R, Johnson SG, Connolly PJ, Wetter SK, Binnun E, Hughes TV, Murray WV, Pandey NB, Moreno-Mazza SJ, Adams M, Fuentes-Pesquera AR, Middleton SA.

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2333-7. doi: 10.1016/j.bmcl.2009.02.067. Epub 2009 Feb 21.

PMID:
19286381
3.

7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: design, synthesis, and biological activity.

Hughes TV, Emanuel SL, O'Grady HR, Connolly PJ, Rugg C, Fuentes-Pesquera AR, Karnachi P, Alexander R, Middleton SA.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5130-3. doi: 10.1016/j.bmcl.2008.07.090. Epub 2008 Jul 26.

PMID:
18718756
4.

4-Amino-6-arylamino-pyrimidine-5-carbaldehyde hydrazones as potent ErbB-2/EGFR dual kinase inhibitors.

Xu G, Abad MC, Connolly PJ, Neeper MP, Struble GT, Springer BA, Emanuel SL, Pandey N, Gruninger RH, Adams M, Moreno-Mazza S, Fuentes-Pesquera AR, Middleton SA.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4615-9. doi: 10.1016/j.bmcl.2008.07.020. Epub 2008 Jul 10.

PMID:
18653333
5.

Discovery of novel 4-amino-6-arylaminopyrimidine-5-carbaldehyde oximes as dual inhibitors of EGFR and ErbB-2 protein tyrosine kinases.

Xu G, Searle LL, Hughes TV, Beck AK, Connolly PJ, Abad MC, Neeper MP, Struble GT, Springer BA, Emanuel SL, Gruninger RH, Pandey N, Adams M, Moreno-Mazza S, Fuentes-Pesquera AR, Middleton SA, Greenberger LM.

Bioorg Med Chem Lett. 2008 Jun 15;18(12):3495-9. doi: 10.1016/j.bmcl.2008.05.024. Epub 2008 May 10.

PMID:
18508264
6.

Cellular and in vivo activity of JNJ-28871063, a nonquinazoline pan-ErbB kinase inhibitor that crosses the blood-brain barrier and displays efficacy against intracranial tumors.

Emanuel SL, Hughes TV, Adams M, Rugg CA, Fuentes-Pesquera A, Connolly PJ, Pandey N, Moreno-Mazza S, Butler J, Borowski V, Middleton SA, Gruninger RH, Story JR, Napier C, Hollister B, Greenberger LM.

Mol Pharmacol. 2008 Feb;73(2):338-48. Epub 2007 Nov 1.

PMID:
17975007
7.

Design, synthesis, and evaluation of 3,4-disubstituted pyrazole analogues as anti-tumor CDK inhibitors.

Lin R, Chiu G, Yu Y, Connolly PJ, Li S, Lu Y, Adams M, Fuentes-Pesquera AR, Emanuel SL, Greenberger LM.

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4557-61. Epub 2007 Jun 6.

PMID:
17574416
8.

Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents.

Lin R, Connolly PJ, Lu Y, Chiu G, Li S, Yu Y, Huang S, Li X, Emanuel SL, Middleton SA, Gruninger RH, Adams M, Fuentes-Pesquera AR, Greenberger LM.

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4297-302. Epub 2007 May 16.

PMID:
17532631
9.

4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation.

Hughes TV, Emanuel SL, Beck AK, Wetter SK, Connolly PJ, Karnachi P, Reuman M, Seraj J, Fuentes-Pesquera AR, Gruninger RH, Middleton SA, Lin R, Davis JM, Moffat DF.

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3266-70. Epub 2007 Apr 10.

PMID:
17481894
10.

Synthesis and biological study of 2-amino-4-aryl-5-chloropyrimidine analogues as inhibitors of VEGFR-2 and cyclin dependent kinase 1 (CDK1).

Huang S, Li R, Connolly PJ, Emanuel S, Fuentes-Pesquera A, Adams M, Gruninger RH, Seraj J, Middleton SA, Davis JM, Moffat DF.

Bioorg Med Chem Lett. 2007 Apr 15;17(8):2179-83. Epub 2007 Feb 2.

PMID:
17317182
11.

The in vitro and in vivo effects of JNJ-7706621: a dual inhibitor of cyclin-dependent kinases and aurora kinases.

Emanuel S, Rugg CA, Gruninger RH, Lin R, Fuentes-Pesquera A, Connolly PJ, Wetter SK, Hollister B, Kruger WW, Napier C, Jolliffe L, Middleton SA.

Cancer Res. 2005 Oct 1;65(19):9038-46.

12.

Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors.

Kuo GH, Prouty C, Wang A, Emanuel S, Deangelis A, Zhang Y, Song F, Beall L, Connolly PJ, Karnachi P, Chen X, Gruninger RH, Sechler J, Fuentes-Pesquera A, Middleton SA, Jolliffe L, Murray WV.

J Med Chem. 2005 Jul 28;48(15):4892-909.

PMID:
16033269
13.

Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.

Kuo GH, Deangelis A, Emanuel S, Wang A, Zhang Y, Connolly PJ, Chen X, Gruninger RH, Rugg C, Fuentes-Pesquera A, Middleton SA, Jolliffe L, Murray WV.

J Med Chem. 2005 Jul 14;48(14):4535-46.

PMID:
15999992
14.

1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.

Lin R, Connolly PJ, Huang S, Wetter SK, Lu Y, Murray WV, Emanuel SL, Gruninger RH, Fuentes-Pesquera AR, Rugg CA, Middleton SA, Jolliffe LK.

J Med Chem. 2005 Jun 30;48(13):4208-11.

PMID:
15974571
15.

3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation.

Lin R, Lu Y, Wetter SK, Connolly PJ, Turchi IJ, Murray WV, Emanuel SL, Gruninger RH, Fuentes-Pesquera AR, Adams M, Pandey N, Moreno-Mazza S, Middleton SA, Jolliffe LK.

Bioorg Med Chem Lett. 2005 May 2;15(9):2221-4.

PMID:
15837297
16.

Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors.

Kuo GH, Wang A, Emanuel S, Deangelis A, Zhang R, Connolly PJ, Murray WV, Gruninger RH, Sechler J, Fuentes-Pesquera A, Johnson D, Middleton SA, Jolliffe L, Chen X.

J Med Chem. 2005 Mar 24;48(6):1886-900.

PMID:
15771433
17.

A vascular endothelial growth factor receptor-2 kinase inhibitor potentiates the activity of the conventional chemotherapeutic agents paclitaxel and doxorubicin in tumor xenograft models.

Emanuel S, Gruninger RH, Fuentes-Pesquera A, Connolly PJ, Seamon JA, Hazel S, Tominovich R, Hollister B, Napier C, D'Andrea MR, Reuman M, Bignan G, Tuman R, Johnson D, Moffatt D, Batchelor M, Foley A, O'Connell J, Allen R, Perry M, Jolliffe L, Middleton SA.

Mol Pharmacol. 2004 Sep;66(3):635-47.

PMID:
15322256

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