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Coumarin-azasugar-b...
Coumarin-azasugar-benzyl conjugates as non-neurotoxic dual inhibitors of butyrylcholinesterase and cancer cell growth
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- Vaaland Holmgard, I. Caroline (författare)
- University of Stavanger, Norway
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- Gonzalez-Bakker, Aday (författare)
- Universidad de La Laguna, Spain
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- Poeta, Eleonora (författare)
- University of Bologna, Italy
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- Puerta, Adrian (författare)
- Universidad de La Laguna, Spain
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- Fernandes, Miguel Xavier (författare)
- Karlstads universitet,Institutionen för ingenjörs- och kemivetenskaper (from 2013)
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- Monti, Barbara (författare)
- University of Bologna, Italy
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- Fernandez-Bolanos, Jose G. (författare)
- Universidad de Sevilla, Spain
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- Padron, Jose M. (författare)
- Universidad de La Laguna, Spain
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- Lopez, Oscar (författare)
- Universidad de Sevilla, Spain
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- Lindback, Emil (författare)
- University of Stavanger, Norway
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(creator_code:org_t)
- Royal Society of Chemistry, 2024
- 2024
- Engelska.
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Ingår i: Organic and biomolecular chemistry. - : Royal Society of Chemistry. - 1477-0520 .- 1477-0539. ; 22:17, s. 3425-3438
- Relaterad länk:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- We have applied the copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction to prepare a library of ten coumarin-azasugar-benzyl conjugates and two phthalimide-azasugar-benzyl conjugates with potential anti-Alzheimer and anti-cancer properties. The compounds were evaluated as cholinesterase inhibitors, demonstrating a general preference, of up to 676-fold, for the inhibition of butyrylcholinesterase (BuChE) over acetylcholinesterase (AChE). Nine of the compounds behaved as stronger BuChE inhibitors than galantamine, one of the few drugs in clinical use against Alzheimer's disease. The most potent BuChE inhibitor (IC50 = 74 nM) was found to exhibit dual activities, as it also showed high activity (GI50 = 5.6 +/- 1.1 mu M) for inhibiting the growth of WiDr (colon cancer cells). In vitro studies on this dual-activity compound on Cerebellar Granule Neurons (CGNs) demonstrated that it displays no neurotoxicity. Coumarin-azasugar-benzyl conjugates were obtained through the CuAAC reaction, displaying dual anti-Alzheimer and anti-cancer activity in vitro and no neurotoxicity.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmakologi och toxikologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmacology and Toxicology (hsv//eng)
Nyckelord
- Kemi
- Chemistry
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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