Výsledky vyhledávání - "Chih-Chung Tseng"

The Trifluoromethyl Group as a Bioisosteric Replacement of the Aliphatic Nitro Group in CB1 Receptor Positive Allosteric Modulators

Autor: Matteo Zanda, Sergio Dall'Angelo, Giulia Donvito, Aron H. Lichtman, Chiara Zanato, Iain R. Greig, Sophie E. Juola, Mohammed A. Mustafa, Ruth A. Ross, Gemma L. Baillie, Chih-Chung Tseng, William T. A. Harrison, Chiara Massarenti

Publikováno v: J Med Chem
Journal of medicinal chemistry 62 (2019): 5049–5062. doi:10.1021/acs.jmedchem.9b00252
info:cnr-pdr/source/autori:Tseng C.-C.; Baillie G.; Donvito G.; Mustafa M.A.; Juola S.E.; Zanato C.; Massarenti C.; Dall'Angelo S.; Harrison W.T.A.; Lichtman A.H.; Ross R.A.; Zanda M.; Greig I.R./titolo:The Trifluoromethyl Group as a Bioisosteric Replacement of the Aliphatic Nitro Group in CB1 Receptor Positive Allosteric Modulators/doi:10.1021%2Facs.jmedchem.9b00252/rivista:Journal of medicinal chemistry/anno:2019/pagina_da:5049/pagina_a:5062/intervallo_pagine:5049–5062/volume:62

The first generation of CB(1) positive allosteric modulators (e.g., ZCZ011) featured a 3-nitroalkyl-2-phenyl-indole structure. Although a small number of drugs include the nitro group, it is generally not regarded as being “drug-like”, and this i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::429df73de2b0a760a53541b1b6887b26
https://doi.org/10.1021/acs.jmedchem.9b00252

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CDP-choline accumulation in breast and colorectal cancer cells treated with a GSK-3-targeting inhibitor

Autor: Su Myat Phyu, Timothy Andrew Davies Smith, Chih-Chung Tseng

Publikováno v: Magma (New York, N.y.)

Purpose Glycogen synthase kinase 3 (GSK3) is a key controlling element of many cellular processes including cell-cycle progression and recent studies suggest that GSK3 is a potential anticancer target. Changes in glucose metabolism associated with GS

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https://doi.org/10.1007/s10334-018-0719-3

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Small Molecule Inhibitors of Metabolic Enzymes Repurposed as a New Class of Anthelmintics

Autor: James W. Janetka, Amarendar Reddy Maddirala, Paul J. Brindley, Judy A. Sakanari, Jonathan D.M. Helander, Iain R. Greig, Scott A. Wildman, Rahul Tyagi, Chih-Chung Tseng, Christina A. Bulman, Mostafa A. Elfawal, Bruce A. Rosa, Makedonka Mitreva, Chelsea Fischer, Xin Gao, Raffi V. Aroian, Mingzhou Zhou, Ryan Chugani

Publikováno v: ACS Infectious Diseases. 4:1130-1145

The enormous prevalence of infections caused by parasitic nematodes worldwide, coupled to the rapid emergence of their resistance to commonly used anthelmintic drugs, presents an urgent need for the discovery of new drugs. Herein, we have identified

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https://doi.org/10.1021/acsinfecdis.8b00090

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Development of Fluorinated Analogues of Perhexiline with Improved Pharmacokinetic Properties and Retained Efficacy

Autor: Monica Sani, Denis M. Grant, Hannah Noordali, Iain R. Greig, Michael P. Frenneaux, Chih-Chung Tseng, Matteo Zanda, Melanie Madhani

Publikováno v: Journal of medicinal chemistry 60 (2017): 2780–2789. doi:10.1021/acs.jmedchem.6b01592
info:cnr-pdr/source/autori:Tseng C.-C.; Noordali H.; Sani M.; Madhani M.; Grant D.M.; Frenneaux M.P.; Zanda M.; Greig I.R./titolo:Development of Fluorinated Analogues of Perhexiline with Improved Pharmacokinetic Properties and Retained Efficacy/doi:10.1021%2Facs.jmedchem.6b01592/rivista:Journal of medicinal chemistry/anno:2017/pagina_da:2780/pagina_a:2789/intervallo_pagine:2780–2789/volume:60

We designed and synthesized perhexiline analogues that have the same therapeutic profile as the parent cardiovascular drug but lacking its metabolic liability associated with CYP2D6 metabolism. Cycloalkyl perhexiline analogues 6a-j were found to be u

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https://doi.org/10.1021/acs.jmedchem.6b01592

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Response Detection of Castrate-Resistant Prostate Cancer to Clinically Utilised and Novel Treatments by Monitoring Phospholipid Metabolism

Autor: Timothy Andrew Davies Smith, Chih-Chung Tseng, K. Alzyoud, Su Myat Phyu

Publikováno v: BioMed Research International
BioMed Research International, Vol 2017 (2017)

Androgen receptor (AR) activation is the primary driving factor in prostate cancer which is initially responsive to castration but then becomes resistant (castration-resistant prostate cancer (CRPC)). CRPC cells still retain the functioning AR which

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Divergent Total Synthesis of Indoxamycins A, C, and F

Autor: Hanfeng Ding, Chi He, Chih-Chung Tseng, Zhifeng Dai, Chenlong Zhu

Publikováno v: Angewandte Chemie International Edition. 52:13256-13260

As a novel class of polyketides, indoxamycins A–F were isolated in 2009 by Sato et al. from saline cultures of marinederived actinomycetes. Within this family, indoxamycins A and F have exhibited promising growth-inhibition activity against HT-29 t

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https://doi.org/10.1002/anie.201307426

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Pyrazole-type cannabinoid ligands conjugated with fluoro-deoxy-carbohydrates as potential PET-imaging agents: Synthesis and CB1/CB2 receptor affinity evaluation

Autor: Gemma L. Baillie, Simona Frau, Paolo Lazzari, Matteo Zanda, Chih-Chung Tseng, Marilena Pira, Ruth A. Ross, Sergio Dall'Angelo

Publikováno v: Journal of fluorine chemistry
152 (2013): 166–172. doi:10.1016/j.jfluchem.2013.03.006
info:cnr-pdr/source/autori:Frau, Simona; Dall'Angelo, Sergio; Baillie, Gemma L.; Ross, Ruth A.; Pira, Marilena; Tseng, Chih-Chung; Lazzari, Paolo; Zanda, Matteo/titolo:Pyrazole-type cannabinoid ligands conjugated with fluoro-deoxy-carbohydrates as potential PET-imaging agents: Synthesis and CB1%2FCB2 receptor affinity evaluation/doi:10.1016%2Fj.jfluchem.2013.03.006/rivista:Journal of fluorine chemistry (Print)/anno:2013/pagina_da:166/pagina_a:172/intervallo_pagine:166–172/volume:152

A novel class of cannabinoid ligands was synthesized in good overall yields by means of oxime-bio-conjugation between hydroxylamine-functionalized Rimonabant-type pyrazoles and fluoro-deoxy-carbohydrates (D-2-fluoro-deoxy-glucose, FDG, and D-5-fluoro

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https://doi.org/10.1016/j.jfluchem.2013.03.006

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Probing the PI3K/Akt/mTor pathway using 31P-NMR spectroscopy: routes to glycogen synthase kinase 3

Autor: Ian N. Fleming, Su Myat Phyu, Chih-Chung Tseng Tseng, Timothy Andrew Davies Smith

Publikováno v: Scientific Reports.

Akt is an intracellular signalling pathway that serves as an essential link between cell surface receptors and cellular processes including proliferation, development and survival. The pathway has many downstream targets including glycogen synthase k

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ChemInform Abstract: Asymmetric Synthesis and Absolute Configuration of (+)- and (-)-Perhexiline

Autor: Matteo Zanda, Iain R. Greig, Chih-Chung Tseng, William T. A. Harrison

Publikováno v: ChemInform. 47

We gratefully thank Signal Pharma for financial support and fellowship (C.C.T), and the EPSRC National Mass Spectrometry Service Centre (Swansea, UK) for performing HRMS analyses. We thank Prof Michael Frenneaux (University of East Anglia, Norwich, U

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https://doi.org/10.1002/chin.201624212

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