Piperidinyl-embeded chalcones possessing anti PI3Kδ inhibitory properties exhibit anti-atopic properties in preclinical models

Dumontet, Charles; Beck, Guillaume; Gardebien, Fabrice; Haudecoeur, Romain; Mathé, Doriane; Matera, Eva–Laure; Tourette, Anne; Mattei, Eve; Esmenjaud, Justine; Boyère, Cédric; Nurisso, Alessandra; Peuchmaur, Marine; Pérès, Basile; Bouchaud, Grégory; Magnan, A.; Monneret, Guillaume; Boumendjel, Ahcène

doi:10.1016/j.ejmech.2018.09.033

Cited by 5 publications

(2 citation statements)

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“…Chalcone derivative 128 was found to inhibit normal basophil degranulation and revealed activity comparable to that of betamethasone as a drug reference (Figure ). A set of chalcone–pyrazine hybrids was constructed and biologically tested. Chalcones with nitro substituents 129 and 130 were effective against Trychophyton mentagrophytes fungi compared with fluconazole as a reference drug.…”

Section: Biological Activities Of Chalcone Derivativesmentioning

confidence: 99%

Synthesis of Chalcones Derivatives and Their Biological Activities: A Review

et al. 2022

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Chalcone derivatives are considered valuable species because they possess a ketoethylenic moiety, CO–CH=CH–. Due to the presence of a reactive α,β-unsaturated carbonyl group, chalcones and their derivatives possess a wide spectrum of antiproliferative, antifungal, antibacterial, antiviral, antileishmanial, and antimalarial pharmacological properties. Recent developments in heterocyclic chemistry have led to the synthesis of chalcone derivatives, which had been biologically investigated toward certain disease targets. The major aspect of this review is to present the most recent synthesis of chalcones bearing N, O, and/or S heterocycles, revealing their biological potential during the past decade (2010–2021). Based on a review of the literature, many chalcone–heterocycle hybrids appear to exhibit promise as future drug candidates owing to their similar or superior activities compared to those of the standards. Thus, this review may prove to be beneficial for the development and design of new potent therapeutic drugs based on previously developed strategies.

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Section: Biological Activities Of Chalcone Derivativesmentioning

confidence: 99%

Synthesis of Chalcones Derivatives and Their Biological Activities: A Review

et al. 2022

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“…Piperidine. Some piperidine tethered chalcone derivatives were synthesized and tested as inhibitors of normal human basophil degranulation and anti-PI3Kδ activities (Dumontet et al, 2018). Compound (16) actively demonstrated to reduce respiratory pressure and inhibit normal human basophil degranulation in a dose-dependent manner.…”

Section: -Membered Ringmentioning

confidence: 99%

Chalcones bearing N, O, and S-heterocycles: Recent notes on their biological significances

2019

J App Pharm Sci

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Because of its relatively easy synthesis, chalcone skeleton has been as a point of interest for organic and medicinal chemists from research groups worldwide. Chalcone scaffold constitutes the core of some interesting biologically active natural products. Chalcone derivatives are among feasible potent active agents, such as anticancer, antibacterial, antifungal, antileishmanial, antimalarial, and antiviral. Due to the knowledge of heterocyclic chemistry, recently chalcones bearing heterocyclic moieties have been synthesized and biologically investigated for specific target of diseases. The current review focuses on the latest application of chalcones integrated with N, O, and S-heterocyclic system and their wide spectrum of biological performance during 10 years (2010)(2011)(2012)(2013)(2014)(2015)(2016)(2017)(2018)(2019). The results reported in the review indicate that many chalcone-heterocycle hybrids may be useful as future drug candidates due to their comparable or higher activity than that of the standards.

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Synthesis of α,β‐Unsaturated Ketones with Secondary Alcohols and Aldehydes Catalyzed by Fe(acac)₃

Zhao

Zhu

et al. 2022

ChemistrySelect

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An efficient and environmentally friendly methodology for the direct synthesis of α,β‐unsaturated ketones by cross‐coupling of secondary alcohols and aldehydes is developed. The transformation is based on Fe(acac)3‐catalyzed Oppenauer oxidation and Claisen‐Schmidt reaction, in which aldehydes are used as oxidants to oxidize secondary alcohols to ketones, and then in situ condensation with aldehydes to form α,β‐unsaturated ketones. The reaction proceeds under base‐free conditions with a wide range of substrates and good compatibility of functional groups. Gram‐scale experiments show the good applicability of this method.

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Piperidinyl-embeded chalcones possessing anti PI3Kδ inhibitory properties exhibit anti-atopic properties in preclinical models

Cited by 5 publications

References 48 publications

Synthesis of Chalcones Derivatives and Their Biological Activities: A Review

Synthesis of Chalcones Derivatives and Their Biological Activities: A Review

Chalcones bearing N, O, and S-heterocycles: Recent notes on their biological significances

Synthesis of α,β‐Unsaturated Ketones with Secondary Alcohols and Aldehydes Catalyzed by Fe(acac)₃

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Piperidinyl-embeded chalcones possessing anti PI3Kδ inhibitory properties exhibit anti-atopic properties in preclinical models

Cited by 5 publications

References 48 publications

Synthesis of Chalcones Derivatives and Their Biological Activities: A Review

Synthesis of Chalcones Derivatives and Their Biological Activities: A Review

Chalcones bearing N, O, and S-heterocycles: Recent notes on their biological significances

Synthesis of α,β‐Unsaturated Ketones with Secondary Alcohols and Aldehydes Catalyzed by Fe(acac)3

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Synthesis of α,β‐Unsaturated Ketones with Secondary Alcohols and Aldehydes Catalyzed by Fe(acac)₃