New amyloid beta-disaggregating agents: synthesis, pharmacological evaluation, crystal structure and molecular docking of<i>N</i>-(4-((7-chloroquinolin-4-yl)oxy)-3-ethoxybenzyl)amines

Umar, Tarana; Shalini, S.; Raza, Kausar; Gusain, Siddharth; Kumar, Jitendra; Ahmed, Waqar; Tiwari, Manisha; Hoda, Nasimul

doi:10.1039/c8md00312b

Cited by 13 publications

(5 citation statements)

References 59 publications

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“…Quinoline, a pharmacophore group, has been extensively used in the synthesis of bioactive compounds against neurodegenerative diseases. In addition, certain quinoline derivatives have been proposed as potential anti-AD agents [ 109 , 110 ]. Ge, Y.X.…”

Section: Resultsmentioning

confidence: 99%

Multi-Target-Directed Cinnamic Acid Hybrids Targeting Alzheimer’s Disease

Drakontaeidi,

Pontiki

2024

IJMS

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Progressive cognitive decline in Alzheimer’s disease (AD) is a growing challenge. Present therapies are based on acetylcholinesterase inhibition providing only temporary relief. Promising alternatives include butyrylcholinesterase (BuChE) inhibitors, multi-target ligands (MTDLs) that address the multi-factorial nature of AD, and compounds that target oxidative stress and inflammation. Cinnamate derivatives, known for their neuroprotective properties, show potential when combined with established AD agents, demonstrating improved efficacy. They are being positioned as potential AD therapeutic leads due to their ability to inhibit Aβ accumulation and provide neuroprotection. This article highlights the remarkable potential of cinnamic acid as a basic structure that is easily adaptable and combinable to different active groups in the struggle against Alzheimer’s disease. Compounds with a methoxy substitution at the para-position of cinnamic acid display increased efficacy, whereas electron-withdrawing groups are generally more effective. The effect of the molecular volume is worthy of further investigation.

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Section: Resultsmentioning

confidence: 99%

Multi-Target-Directed Cinnamic Acid Hybrids Targeting Alzheimer’s Disease

Drakontaeidi,

Pontiki

2024

IJMS

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“…The metal binding studies were performed as described in [ 58 ]. The UV absorption of the LBE (500 μg/mL) alone or in the presence of CuSO 4 , FeSO 4, or FeCl 3 (40 μM) for 30 min in 20% ( v / v ) ethanol/buffer (20 mM HEPES, 150 mM NaCl, pH 7.4) was recorded using a microplate reader (Multiskan Go, Thermo Scientific, Waltham, MA, USA) with a wavelength ranging from 280 to 400 nm.…”

Section: Methodsmentioning

confidence: 99%

Anticancer Therapies Based on Oxidative Damage: Lycium barbarum Inhibits the Proliferation of MCF-7 Cells by Activating Pyroptosis through Endoplasmic Reticulum Stress

Miranda,

Basilicata,

Vestuto

et al. 2024

Antioxidants

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Lycium barbarum, commonly recognized as goji berry or wolfberry, is highly appreciated not only for its organoleptic and nutritional properties but also as an important source of bioactive compounds such as polysaccharides, carotenoids, phenolics, and various other non-nutritive compounds. These constituents give it a multitude of health benefits, including antioxidant, anti-inflammatory, and anticancer properties. However, the precise biochemical mechanisms responsible for its anticancer effects remain unclear, and the comprehensive composition of goji berry extracts is often insufficiently explored. This study aimed to investigate the biochemical pathways modulated in breast cancer cells by an ethanolic extract of Lycium barbarum fruit (LBE). Following metabolomic profiling using UHPLC-HRMS/MS, we assessed the antitumoral properties of LBE on different breast cancer cell lines. This investigation revealed that LBE exhibited cytotoxic effects, inducing a pro-oxidant effect that triggered pyroptosis activation through endoplasmic reticulum (ER) stress and subsequent activation of the P-IRE1α/XBP1/NLRP3 axis in MCF-7 cells. In addition, LBE did not display cytotoxicity toward healthy human cells but demonstrated antioxidant properties by neutralizing ROS generated by doxorubicin. These findings underscore the potential of LBE as a highly promising natural extract in cancer therapy.

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“…In accordance with the amyloid‐β cascade, hypothesis of AD brain aggregation of amyloid‐β starts the disease process. The drug research holds amyloid‐β production, deposition and clearance as the therapeutic strategies (Economou et al, 2016; Labouze et al, 2015; Umar, Shalini, Raza, Gusain, Kumar, Seth, Ahmed, et al, 2019). This hypothesis suggests that degeneration of amyloid‐β, procured from APP via β‐ and γ‐secretase, is reduced by age or pathological conditions, which triggers aggregation of amyloid‐β peptides (Aβ 40 and Aβ 42 ).…”

Section: Primary Drug Therapies For Admentioning

confidence: 99%

Recent updates in the development of small molecules as potential clinical candidates for Alzheimer's disease: A review

et al. 2022

Self Cite

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Alzheimer's disease (AD) is one of the prominent causes for disability and lowered quality of life worldwide in elderly population. It has fostered immense burden to AD patients, families and society. Burgeoning progress in the field of pathogenesis over last two decades has persuaded the investigation of novel pharmacological therapeutics that focuses towards the pathophysiological events of AD. Miscellaneous clinical trials, development and testing of interventions aimed at various targets, such as anti-tau and anti-amyloid interventions, neurotransmitter modification, neuroprotection and anti-neuroinflammation interventions, cognitive enhancement and interventions to palliate behavioural symptoms have been carried out. Despite massive efforts to find disease-modifying therapies,there lingers a vital need for continuing the advancement in progress of the AD research. This review features the new developments of small molecule compounds that will be beneficial in evolution of new AD therapies. In particular, this review briefly describes summary of mechanistic causes chiefly associated with AD and focuses on medicinal approach via small molecule inhibitors that can manage cognitive impairment and dysfunction and may combat Alzheimer's development.

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New amyloid beta-disaggregating agents: synthesis, pharmacological evaluation, crystal structure and molecular docking ofN-(4-((7-chloroquinolin-4-yl)oxy)-3-ethoxybenzyl)amines

Abstract: N-(4-((7-Chloroquinolin-4-yl)oxy)-3-ethoxybenzyl)amines as new amyloid beta-disaggregating agents.

Cited by 13 publications

References 59 publications

Multi-Target-Directed Cinnamic Acid Hybrids Targeting Alzheimer’s Disease

Multi-Target-Directed Cinnamic Acid Hybrids Targeting Alzheimer’s Disease

Anticancer Therapies Based on Oxidative Damage: Lycium barbarum Inhibits the Proliferation of MCF-7 Cells by Activating Pyroptosis through Endoplasmic Reticulum Stress

Recent updates in the development of small molecules as potential clinical candidates for Alzheimer's disease: A review

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