Výsledky vyhledávání - "Candy Robinson"

Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders

Autor: Elizabeth O. Hexner, Thelma S. Angeles, Pawel Dobrzanski, Cynthia Serdikoff, Martin Carroll, Mahfuza Jan, Bruce Ruggeri, Shi Yang, Stephen G. Emerson, Cezary R. Swider, Candy Robinson

Publikováno v: Blood. 111:5663-5671

Recent studies have demonstrated that patients with myeloproliferative disorders (MPDs) frequently have acquired activating mutations in the JAK2 tyrosine kinase. A multikinase screen determined that lestaurtinib (formerly known as CEP-701) inhibits

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::190d6a9ee41147ee11e8fc75c67873c0
https://doi.org/10.1182/blood-2007-04-083402

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Design and synthesis of dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole oximes as potent dual inhibitors of TIE-2 and VEGF-R2 receptor tyrosine kinases

Autor: Edward R. Bacon, Robert L. Hudkins, Thelma S. Angeles, Jennifer Grobelny, Mark S. Albom, Reddeppareddy Dandu, Bruce Ruggeri, Sheila J. Miknyoczki, Lisa D. Aimone, Shi Yang, Candy Robinson, Hong Chang, Allison L. Zulli, Ted L. Underiner

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:1916-1921

Fused dihydroindazolopyrrolocarbazole oximes have been identified as low nanomolar, potent dual TIE-2 and VEGF-R2 receptor tyrosine kinase inhibitors with excellent cellular potency. Development of the structure-activity relationships (SAR) led to id

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff81dd5bd91b90c842800ca27629d74b
https://doi.org/10.1016/j.bmcl.2008.02.001

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Novel C-3 N-urea, amide, and carbamate dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs as potent TIE-2 and VEGF-R2 dual inhibitors

Autor: Allison L. Zulli, Lisa D. Aimone, Robert L. Hudkins, Nadine C. Becknell, Mark S. Albom, Thelma S. Angeles, Candy Robinson, Hong Chang, Shi Yang

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:5368-5372

A novel series of C-3 urea, amide, and carbamate fused dihydroindazolocarbazole (DHI) analogs are reported as highly potent dual inhibitors of TIE-2 and VEGF-R2 receptor tyrosine kinases with excellent cellular potency. Structure-activity relationshi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::be20e050136bda1b5252fe5bfa04cc2f
https://doi.org/10.1016/j.bmcl.2006.07.066

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THE CHARACTERIZATION OF POTENT NOVEL WARFARIN ANALOGS

Autor: Janet S Kerr, Andrea J. Robinson, Candy Robinson, Hui-Yin Li, Roseanne S Wexler, George A. Boswell, Candice M. Krauthauser, Patricia P Harlow

Publikováno v: Thrombosis Research. 88:127-136

Racemic sodium warfarin, Coumadin,® is widely used in the prevention of thromboembolic disease. The present study was undertaken to characterize three novel classes of warfarin analogs, and to compare them with the warfarin enantiomers. All three cl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::47ac65442485854a4bf48d00649aaaea
https://doi.org/10.1016/s0049-3848(97)00224-7

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Design, synthesis and structure-activity relationship studies of novel 4,4-bis(trifluoromethyl)imidazolines as acyl-CoA: Cholesterol acyltransferase (ACAT) inhibitors and antihypercholesterolemic agents

Autor: Spencer Drummond, George A. Boswell, Candy Robinson, Hui-Yin Li, Peter J. Gillies, Jeffrey T. Billheimer, Indawati Delucca

Publikováno v: Bioorganic & Medicinal Chemistry. 5:1345-1361

Novel 4,4-bis(trifluoromethyl)imidazolines have been found to be the potent acyl-CoA cholesterol acyltransferase (ACAT) inhibitors. ACAT is responsible for cholesterol esterification in the intestine, liver, and the arterial wall. These novel imidazo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eb7434ea6261df1bf049dcdf56be5ecc
https://doi.org/10.1016/s0968-0896(97)00058-8

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TIE-2/VEGF-R2 SAR and in vitro activity of C3-acyl dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs

Autor: Lisa D. Aimone, Kurt A. Josef, Linda Weinberg, Mark S. Albom, Shi Yang, Allison L. Zulli, Robert L. Hudkins, Thelma S. Angeles, Bruce Ruggeri, Kathryn Hunter, Ted L. Underiner, Candy Robinson, Hong Chang

Publikováno v: Bioorganicmedicinal chemistry letters. 18(7)

Orally bioavailable, dual inhibitors of TIE-2/VEGF-R2 were identified by elaborating the C3/N13 SAR around a fused pyrrolodihydroindazolocarbazole scaffold. Analogs bearing a C3-thiophencarbonyl group were evaluated in enzymatic and cellular biochemi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c5b4e3bad205bc67fb6921428813f3c
https://pubmed.ncbi.nlm.nih.gov/18343109

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Structure-guided identification of novel VEGFR-2 kinase inhibitors via solution phase parallel synthesis

Autor: Shi X. Yang, Mark S. Albom, Thelma S. Angeles, Mohamed Iqbal, Candy Robinson, Hong Chang, John P. Mallamo, Alyssa Reiboldt, Rabindranath Tripathy, Bruce Ruggeri, Edward R. Bacon, Patricia A. Messina, Jasbir Singh

Publikováno v: Bioorganicmedicinal chemistry letters. 16(8)

Structural analysis of the essential binding elements of the oxindole-based kinase inhibitor (1) led to the identification of a novel class of heterocyclic-substituted pyrazolones. Knoevenagel condensation of a variety of activated methylene nucleoph

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6e308ce3ec908f1045b8ab0dfd25e327
https://pubmed.ncbi.nlm.nih.gov/16460933

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Antiangiogenic and antitumor efficacy of EphA2 receptor antagonist

Autor: Hugh Zhao, Hong Chang, Susan Jones-Bolin, Pawel Dobrzanski, Candy Robinson, Bruce Ruggeri, Kathryn Hunter, Sonya Pritchard

Publikováno v: Cancer research. 64(3)

Tumor-associated angiogenesis is critical for tumor growth and metastasis and is controlled by various pro- and antiangiogenic factors. The Eph family of receptor tyrosine kinases has emerged as one of the pivotal regulators of angiogenesis. Here we

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::efa2aadc64edd1b9c27d30b15f5af080
https://pubmed.ncbi.nlm.nih.gov/14871820

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The chemopreventive agent oltipraz possesses potent antiangiogenic activity in vitro, ex vivo, and in vivo and inhibits tumor xenograft growth

Autor: Bruce A, Ruggeri, Candy, Robinson, Thelma, Angeles, John, Wilkinson, Margie L, Clapper

Publikováno v: Clinical cancer research : an official journal of the American Association for Cancer Research. 8(1)

Angiogenesis plays a pivotal role in tumor growth and represents a key target for chemopreventive intervention. On the basis of the structural features and lack of target organ specificity of the synthetic dithiolethione oltipraz, inhibition of angio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::4e615dd0336452e693fe5cd2f7b8a93e
https://pubmed.ncbi.nlm.nih.gov/11801568

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