Výsledky vyhledávání - "Jeanelle McSurdy-Freed"

[3a,4]-Dihydropyrazolo[1,5a]pyrimidines: Novel, Potent, and Selective Phosphatidylinositol-3-kinase β Inhibitors

Autor: Michael D. Spengler, Ramona Plant, Kaushik Raha, Hong Lin, Hongyi Yu, Cynthia M. Rominger, Ralph A. Rivero, Michael L. Moore, Mary Ann Hardwicke, Michael D. Schaber, Jeanelle McSurdy-Freed, Karl F. Erhard, Juan I. Luengo, Junya Qu

Publikováno v: ACS Medicinal Chemistry Letters. 4:230-234

A series of novel [3a,4]dihydropyrazolo[1,5a]pyrimidines were identified, which were highly potent and selective inhibitors of PI3Kβ. The template afforded the opportunity to develop novel SAR for both the hinge-binding (R3) and back-pocket (R4) sub

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::57afc57af006ff9d145d664dbb899011
https://doi.org/10.1021/ml300330m

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Differences in Effects on Myocardium and Mitochondria by Angiogenic Inhibitors Suggest Separate Mechanisms of Cardiotoxicity

Autor: Shufang Zhao, Laura M. Storck, Charles B. Davis, Jeanelle McSurdy-Freed, Robert W. Coatney, Kendall S. Frazier, Catherine X. Hu, Jon Renninger, Tracy L. Gales, Kevin French, Emile Chen

Publikováno v: Toxicologic Pathology. 38:691-702

Several multikinase angiogenesis inhibitors demonstrate mitochondrial and/or cardiovascular toxicity, suggesting an on-target pharmacologic effect. To evaluate whether cardiotoxicity is directly related to vascular endothelial growth factor receptor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff8d4a5772d8c94ac8da7b11bb9b9753
https://doi.org/10.1177/0192623310373775

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Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors

A novel thiazolopyrimidinone series of PI3K-beta selective inhibitors has been identified. This chemotype has provided an excellent tool compound, 18, that showed potent growth inhibition in the PTEN-deficient breast cancer cell line MDA-MB-468 under

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ace88350b0677b6d5e549d1aab456577
https://europepmc.org/articles/PMC4025772/

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Synthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potent β isoform selective phosphatidylinositol 3-kinase inhibitors

Autor: Sanchez Robert, Jeanelle McSurdy-Freed, Hongyi Yu, Michael L. Moore, Rosanna Tedesco, Mary Ann Hardwicke, Karl F. Erhard, Ralph A. Rivero, Kaushik Raha, Michael D. Spengler, Juan I. Luengo, Ramona Plant, Hong Lin, Michael D. Schaber, Cynthia M. Rominger

Publikováno v: Bioorganicmedicinal chemistry letters. 22(9)

A series of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones with excellent enzyme inhibition, improved isoform selectivity, and excellent inhibition of downstream phosphorylation of AKT has been identified. Several compounds in the series demonstrated pote

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::39aeedab2fa3b426ab69e2e507b41350
https://pubmed.ncbi.nlm.nih.gov/22475557

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Synthesis and structure-activity relationships of imidazo[1,2-a]pyrimidin-5(1H)-ones as a novel series of beta isoform selective phosphatidylinositol 3-kinase inhibitors

Autor: Michael D. Spengler, Rosanna Tedesco, Sanchez Robert, Michael D. Schaber, Ramona Plant, Hong Lin, Mary Ann Hardwicke, Karl F. Erhard, James F. Mack, Kaushik Raha, Ralph A. Rivero, Cynthia M. Rominger, Juan I. Luengo, Mark J. Schulz, Jeanelle McSurdy-Freed, Ren Xie, Jin J. Zeng

Publikováno v: Bioorganicmedicinal chemistry letters. 22(6)

A series of PI3K-beta selective inhibitors, imidazo[1,2-a]-pyrimidin-5(1H)-ones, has been rationally designed based on the docking model of the more potent R enantiomer of TGX-221, identified by a chiral separation, in a PI3K-beta homology model. Syn

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a88dac9bc6de289344a6d52a979b9376
https://pubmed.ncbi.nlm.nih.gov/22361133

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Preclinical drug metabolism and pharmacokinetic evaluation of GW844520, a novel anti-malarial mitochondrial electron transport inhibitor

Autor: Ramesh Bambal, Hong Xiang, Jeanelle McSurdy-Freed, Ganesh S. Moorthy, Charles B. Davis, Erin D. Hugger, Chao Han, Santiago Ferrer, Domingo Gargallo

Publikováno v: Journal of pharmaceutical sciences. 95(12)

GW844520 is a potent and selective inhibitor of the cytochrome bc1 complex of mitochondrial electron transport in P. falciparum, the parasite primarily responsible for the mortality associated with malaria worldwide. GW844520 is fully active against

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9775367176698713e3a4665f1391eeee
https://pubmed.ncbi.nlm.nih.gov/16892205

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Abstract 5418: Rapid LDH5 inhibition reverses malignant metabolic phenotype and impairs survival of hepatocellular carcinoma cells

Publikováno v: Cancer Research. 73:5418-5418

Many cancer cells generate energy by rapidly converting glucose to lactate in the cytosol, a process termed aerobic glycolysis. This metabolic phenotype is recognized as one of the hallmarks of cancer and is enabled by lactate dehydrogenase (LDH), wh

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::576a51c8e9d9033c2f66c0893f65562a
https://doi.org/10.1158/1538-7445.am2013-5418

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Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells

Publikováno v: Cancer & Metabolism

Background Most normal cells in the presence of oxygen utilize glucose for mitochondrial oxidative phosphorylation. In contrast, many cancer cells rapidly convert glucose to lactate in the cytosol, a process termed aerobic glycolysis. This glycolytic

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