Výsledky vyhledávání - "Ted L. Underiner"

2,4-Diaminopyrimidine inhibitors of c-Met kinase bearing benzoxazepine anilines

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:660-663

Elaboration of the SAR around a series of 2,4-diaminopyrimidines led to a number of c-Met inhibitors in which kinase selectivity was modulated by substituents appended on the C4-aminobenzamide ring and the nature of the C2-aminoaryl ring. Further lea

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cd2f5ede7c3bb696001314f924df06f4
https://doi.org/10.1016/j.bmcl.2010.12.013

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Synthesis and structure–activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase

Autor: Linda Weinberg, Ted L. Underiner, Mark S. Albom, Craig A. Zificsak, Arup K. Ghose, Renee C. Roemmele, Mangeng Cheng, Karen L. Milkiewicz, Jay P. Theroff, Bruce D. Dorsey, Thelma S. Angeles

Publikováno v: Bioorganic & Medicinal Chemistry. 18:4351-4362

Dysregulation of the anaplastic lymphoma kinase (ALK) is implicated in a variety of cancers. A series of tetrahydropyrido[2,3-b]pyrazines was constructed as ring-constrained analogs of a known aminopyridine kinase scaffold. Chemistry was developed to

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b1bddc45e141f6cd00dccf8a2e98b12a
https://doi.org/10.1016/j.bmc.2010.04.087

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Discovery of Small Molecule c-Met Inhibitors: Evolution and Profiles of Clinical Candidates

Autor: Sheila J. Miknyoczki, Torsten Herbertz, Ted L. Underiner

Publikováno v: Anti-Cancer Agents in Medicinal Chemistry. 10:7-27

The scatter factor/hepatocyte growth factor (HGF)-c-Met axis is involved in the malignant phenotype of various tumor types via activation of a wide range of autocrine and paracrine processes. Autocrine activation of tumor cell c-Met receptors enhance

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7a06afc09f2777a1329ec565f923b48a
https://doi.org/10.2174/1871520611009010007

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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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CT2108A and B: New Fatty Acid Synthase Inhibitors as Antifungal Agents

Autor: Ursula Mocek, Ted L. Underiner, Sheldon E. Broedel, Gail E. McElhaney-Feser, Robert E. Raulli, Jodi A. Laakso, Paul Actor, Brian J. Hotovec, Ronald L. Cihlar

Publikováno v: Journal of Natural Products. 66:1041-1046

A systematic screen for new natural products that displayed antifungal activity by inhibition of fungal fatty acid synthase (FAS) led to the discovery of two new fungal metabolites, designated CT2108A (1) and CT2108B (2). The metabolites were produce

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed488c143650a930af65d96c4a156141
https://doi.org/10.1021/np030046g

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Solution Phase Synthesis of Chemical Libraries for Lead Discovery

Autor: Richard D. Cramer, Allan M. Ferguson, Ted L. Underiner, Cheryl D. Garr, Michael S. Lawless, Lauri Schultz, John R. Peterson, David E. Patterson, Amy Oliver

Publikováno v: SLAS Discovery. 1:179-186

By integrating advanced computational design and synthesis, a series of structurally diverse reaction products based on three core scaffolds were prepared by a propietary high throughput synthesis method. Incorporation of auto-mated work stations and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::06866471cbd1b59e54bf932d19ae84fa
https://doi.org/10.1177/108705719600100404

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Designing Chemical Libraries for Lead Discovery

Autor: David E. Patterson, Allan M. Ferguson, Cheryl D. Garr, Ted L. Underiner

Publikováno v: SLAS Discovery. 1:65-73

The selection of compounds for use in high throughput biological assays is one of the critical factors that dictates the likelihood of detecting exploitable biological properties. In this paper, we present a process designed to deliver molecules that

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::bc56f0fd04d6229be2ad518deb05ef86
https://doi.org/10.1177/108705719600100204

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Improvement of inhibitor identification for heat shock protein 90α by utilizing a red-shifted fluorescence polarization probe

Autor: Ted L. Underiner, Sheryl L. Meyer, Beverly P. Holskin, Thelma S. Angeles, Jay P. Theroff, Jie Qian

Publikováno v: Assay and drug development technologies. 10(4)

Heat shock protein-90 (HSP90) is an ATP-dependent molecular chaperone with intrinsic ATPase activity. HSP90 is required for the stability and function of client proteins, many of which are involved in oncogenesis. Thus, identification of HSP90 inhibi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::55bc3c1fcd0722ed37fdab3a82a4e043
https://pubmed.ncbi.nlm.nih.gov/22428803

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