Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease

Huang, Ling; Miao, Hui; Sun, Yang; Meng, Fanchao; Li, Xingshu

doi:10.1016/j.ejmech.2014.09.081

Cited by 63 publications

(59 citation statements)

References 41 publications

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“…It is noteworthy that 2-(1H-pyrazol-1-yl)-thiazole derivatives, which possess a conformationally constrained scaffold, similar to the one envisaged in this work, exhibited a potent EP1 receptor antagonist profile [19]. Additionally, a noticeable number of indanone derivatives constitute lead compounds for the treatment of Alzheimer's disease [20]. Therefore, it is apparent from bibliography that fused pyrazoles can display pronounced biological activities, and their further exploitation should be a constant goal of medicinal chemists.…”

Section: Introductionmentioning

confidence: 64%

Novel conformationally constrained pyrazole derivatives as potential anti-cancer agents

Kasiotis

Tzanetou

Stagos

et al. 2015

Zeitschrift Für Naturforschung B

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The synthesis of 17 novel conformationally constrained pyrazole derivatives is reported herein, along with the assessment of their anti-proliferative and antiangiogenic activities. The evaluation of their inhibitory effect on cell proliferation against HepG2, HeLa, and MCF-7 cells revealed the pyrrolo[2,3-g]indazole 23 as a potent inhibitor of cell growth with IC 50 values of 5 μm. Additionally, the inhibition of vascular endothelial growth factor by pyrazoles 20 and 23 (30 % and 35 %, respectively) in HeLa supernatant cells was evidenced. These findings highlight the usefulness of these compounds as potential scaffolds for the design and development of novel anticancer agents with pronounced anti-angiogenic activity.

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Section: Introductionmentioning

confidence: 64%

Novel conformationally constrained pyrazole derivatives as potential anti-cancer agents

Kasiotis

Tzanetou

Stagos

et al. 2015

Zeitschrift Für Naturforschung B

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“…To determine the inhibitory activities of these target compounds against AChE and BuChE, IC 50 of all compounds was obtained. Lead compound 1 and donepezil were used as the reference compounds, and the results are shown in Table .…”

Section: Resultsmentioning

confidence: 99%

Design, synthesis, biological evaluation, and docking study of 4‐isochromanone hybrids bearing N‐benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II)

Wang

Zheng

et al. 2017

Chem Biol Drug Des

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A series of novel 4-isochromanone compounds bearing N-benzyl pyridinium moiety were designed and synthesized as acetylcholinesterase (AChE) inhibitors. The biological evaluation showed that most of the target compounds exhibited potent inhibitory activities against AChE. Among them, compound 1q possessed the strongest anti-AChE activity with an IC value of 0.15 nm and high AChE/BuChE selectivity (SI > 5,000). Moreover, compound 1q had low toxicity in normal nerve cells and was relatively stable in rat plasma. Together, the current finding may provide a new approach for the discovery of novel anti-Alzheimer's disease agents.

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“…New 1-indanone derivatives that may be used as multi-functional drugs for the treatment of Alzheimer's disease have been synthesized by Li et al [8]. In this synthesis, ferulic acid ( 23 ) was hydrogenated in the presence of Pd/C catalyst to give the saturated derivative 24 and then cyclized to the 1-indanone 25 .…”

Section: Reviewmentioning

confidence: 99%

“…In addition, structurally related indanes also showed biological activity and have been reviewed by Ahmed in 2016 [4]. Extensive studies on bioactivity of 1-indanone derivatives open up more and more new possibilities of their applications as antiviral and antibacterial agents [5] ( I and II ), anticancer drugs [6] ( VI ), pharmaceuticals used in the Alzheimer’s disease treatment [7] ( III ), cardiovascular drugs [7] ( IV ), insecticides, fungicides, herbicides [8] ( V ) and non-nucleoside, low molecular drugs for the hepatitis C treatment, which inhibit HCV replication [9–10] (Fig. 1).…”

Section: Introductionmentioning

confidence: 99%

Synthesis of 1-indanones with a broad range of biological activity

Turek¹,

Szczęsna²,

Koprowski³

et al. 2017

Beilstein J. Org. Chem.

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This comprehensive review describes methods for the preparation of 1-indanones published in original and patent literature from 1926 to 2017. More than 100 synthetic methods utilizing carboxylic acids, esters, diesters, acid chlorides, ketones, alkynes, alcohols etc. as starting materials, have been performed. This review also covers the most important studies on the biological activity of 1-indanones and their derivatives which are potent antiviral, anti-inflammatory, analgesic, antimalarial, antibacterial and anticancer compounds. Moreover, they can be used in the treatment of neurodegenerative diseases and as effective insecticides, fungicides and herbicides.

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Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease

Cited by 63 publications

References 41 publications

Novel conformationally constrained pyrazole derivatives as potential anti-cancer agents

Novel conformationally constrained pyrazole derivatives as potential anti-cancer agents

Design, synthesis, biological evaluation, and docking study of 4‐isochromanone hybrids bearing N‐benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II)

Synthesis of 1-indanones with a broad range of biological activity

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