Výsledky vyhledávání - "Angel R. Fuentes-Pesquera"

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

Autor: Peter J. Connolly, Jonathan M. Blevitt, Virna B. Borowski, Kenneth R. LaMontagne, Jeannene Butler, Lee M. Greenberger, Shenlin Huang, Angel R. Fuentes-Pesquera, Ronghua Li

Publikováno v: Angiogenesis. 12:287-296

Angiogenesis is a complex process that relies on a variety of growth factors and signaling pathways to stimulate endothelial cell responses and establish functional blood vessels. Signaling through the vascular endothelial growth factor (VEGF) recept

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf20bc6380d79aad70b725dbb2bb4bf0
https://doi.org/10.1007/s10456-009-9151-7

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

Autor: Catherine A. Rugg, Angel R. Fuentes-Pesquera, Steven A. Middleton, Stuart Emanuel, Peter J. Connolly, Richard S. Alexander, Terry V. Hughes, Prabha Karnachi, Harold R. O’Grady

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:5130-5133

A novel series of 7-[1H-indol-2-yl]-2,3-dihydro-isoindol-1-ones designed to be inhibitors of VEGF-R2 kinase was synthesized and found to potently inhibit VEGF-R2 and Aurora-A kinases. The structure-based design, synthesis, and initial SAR of the seri

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::74affa60ae9f6997d3605a0b25abe5da
https://doi.org/10.1016/j.bmcl.2008.07.090

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

Autor: Yanhua Lu, Lee M. Greenberger, George Chiu, Yang Yu, Angel R. Fuentes-Pesquera, Peter J. Connolly, Steven A. Middleton, Mary Adams, Stuart Emanuel, Shenlin Huang, Xun Li, Ronghui Lin, Shengjian Li, Robert H. Gruninger

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 17:4297-4302

A series of 3,5-disubstituted pyrazolo[3,4-b]pyridine cyclin-dependent kinase (CDK) inhibitors was synthesized. These compounds showed potent and selective CDK inhibitory activities and inhibited in vitro cellular proliferation in cultured human tumo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a8f2d48728d83c8edb087787289e23ed
https://doi.org/10.1016/j.bmcl.2007.05.029

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

Autor: Ronghua Li, Angel R. Fuentes-Pesquera, David Festus Charles Moffat, Jeremy Martin Davis, Peter J. Connolly, Steven A. Middleton, Mary Adams, Stuart Emanuel, Jabed Seraj, Robert H. Gruninger, Shenlin Huang

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 17:2179-2183

The series of 2-amino-4-aryl-5-chloropyrimidines was discovered to be potent for both VEGFR-2 and CDK1. Described here are the chemistry for analogue synthesis, SAR study, and its kinase selectivity prolifing. The full rat PK data and in vivo efficac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2a06a3d846771b7f6a3abe42236fc71a
https://doi.org/10.1016/j.bmcl.2007.01.086

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The In vitro and In vivo Effects of JNJ-7706621: A Dual Inhibitor of Cyclin-Dependent Kinases and Aurora Kinases

Autor: Cheryl Napier, Angel R. Fuentes-Pesquera, Steven K. Wetter, Beth A. Hollister, Linda K. Jolliffe, Steven A. Middleton, Peter J. Connolly, Catherine A. Rugg, Robert H. Gruninger, Ronghui Lin, Walter W. Kruger, Stuart Emanuel

Publikováno v: Cancer Research. 65:9038-9046

Modulation of aberrant cell cycle regulation is a potential therapeutic strategy applicable to a wide range of tumor types. JNJ-7706621 is a novel cell cycle inhibitor that showed potent inhibition of several cyclin-dependent kinases (CDK) and Aurora

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a88ed898d25c1adfd6adc05dacb83221
https://doi.org/10.1158/0008-5472.can-05-0882

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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

Autor: Stuart Emanuel, Yanhua Lu, Ronghui Lin, Shenlin Huang, Linda Jolliffe, Steven A. Middleton, Robert H. Gruninger, Peter J. Connolly, Steven K. Wetter, William V. Murray, Catherine A. Rugg, Angel R. Fuentes-Pesquera

Publikováno v: Journal of Medicinal Chemistry. 48:4208-4211

A series of 1-acyl-1H-[1,2,4]triazole-3,5-diamine analogues were synthesized as cyclin-dependent kinase (CDK) inhibitors. These compounds showed potent and selective CDK1 and CDK2 inhibitory activities and inhibited in vitro cellular proliferation in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::84da515c0c38880abe4a77c7d8880429
https://doi.org/10.1021/jm050267e

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Synthesis and Identification of [1,3,5]Triazine-pyridine Biheteroaryl as a Novel Series of Potent Cyclin-Dependent Kinase Inhibitors

Autor: Angel R. Fuentes-Pesquera, Steven A. Middleton, Aihua Wang, Yan Zhang, Catherine A. Rugg, Robert H. Gruninger, William V. Murray, Linda Jolliffe, Stuart Emanuel, Alan Deangelis, Peter J. Connolly, Xin Chen, Gee-Hong Kuo

Publikováno v: Journal of Medicinal Chemistry. 48:4535-4546

On the basis of previous studies, we identified pyrazine-pyridine A as a potent vascular endothelial growth factor inhibitor and pyrimidine-pyridine B as a moderately potent cyclin dependent kinase (CDK) inhibitor. A proposed combination of CGP-60474

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f007997c283ae12c9cd0ec2727352d16
https://doi.org/10.1021/jm040214h

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Synthesis and Discovery of Pyrazine−Pyridine Biheteroaryl as a Novel Series of Potent Vascular Endothelial Growth Factor Receptor-2 Inhibitors

Autor: Xin Chen, Gee-Hong Kuo, Linda Jolliffe, Robert H. Gruninger, Angel R. Fuentes-Pesquera, Steven A. Middleton, Dana L. Johnson, Aihua Wang, Rui Zhang, Stuart Emanuel, William V. Murray, Peter J. Connolly, Alan Deangelis, Jan L. Sechler

Publikováno v: Journal of Medicinal Chemistry. 48:1886-1900

Pathological angiogenesis is associated with disease states such as cancer, diabetic retinopathy, rheumatoid arthritis, endometriosis, and psoriasis. There is much evidence that direct inhibition of the kinase activity of vascular endothelial growth

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bd40f4ab5441260d73eeb1de9fe7ad5d
https://doi.org/10.1021/jm040099a

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

Autor: Niranjan Pandey, Angel R. Fuentes-Pesquera, Eva Binnun, Sigmond G. Johnson, Steven K. Wetter, Sandra Moreno-Mazza, Terry V. Hughes, William V. Murray, Steven A. Middleton, Peter J. Connolly, Ronghui Lin, Mary Adams

Publikováno v: Bioorganicmedicinal chemistry letters. 19(8)

2,7-Diamino-thiazolo[4,5-d]pyrimidine analogues were synthesized as novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. Representative compounds showed potent and selective EGFR inhibitory activities and inhibited in vitro cellu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::482987d90be9b720be65b623859b5211
https://pubmed.ncbi.nlm.nih.gov/19286381

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