Chalcone Derivatives: Promising Starting Points for Drug Design.
Marcelo N. Gomes,Eugene N. Muratov,Maristela Pereira,Josana de Castro Peixoto,Lucimar Pinheiro Rosseto,Pedro Cravo,Carolina Horta Andrade,Bruno J. Neves,Bruno J. Neves +8 more
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TLDR
This review summarizes current methodological developments towards the design and synthesis of new chalcone derivatives and state-of-the-art medicinal chemistry strategies (bioisosterism, molecular hybridization, and pro-drug design) and presents successful examples of the use of chalcones.Abstract:
Medicinal chemists continue to be fascinated by chalcone derivatives because of their simple chemistry, ease of hydrogen atom manipulation, straightforward synthesis, and a variety of promising biological activities. However, chalcones have still not garnered deserved attention, especially considering their high potential as chemical sources for designing and developing new effective drugs. In this review, we summarize current methodological developments towards the design and synthesis of new chalcone derivatives and state-of-the-art medicinal chemistry strategies (bioisosterism, molecular hybridization, and pro-drug design). We also highlight the applicability of computer-assisted drug design approaches to chalcones and address how this may contribute to optimizing research outputs and lead to more successful and cost-effective drug discovery endeavors. Lastly, we present successful examples of the use of chalcones and suggest possible solutions to existing limitations.read more
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Pharmacological Properties of Chalcones: A Review of Preclinical Including Molecular Mechanisms and Clinical Evidence.
Bahare Salehi,Cristina Quispe,Imane Chamkhi,Nasreddine El Omari,Abdelaali Balahbib,Javad Sharifi-Rad,Abdelhakim Bouyahya,Muhammad Akram,Mehwish Iqbal,Anca Oana Docea,Constantin Caruntu,Gerardo Leyva-Gómez,Abhijit Dey,Miquel Martorell,Daniela Calina,Víctor López,Francisco Les +16 more
TL;DR: In this article, a review comprehensively describes preclinical studies on chalcones and their derivatives describing their immense significance as antidiabetic, anticancer, anti-inflammatory, antimicrobial, antioxidant, antiparasitic, psychoactive, and neuroprotective agents.
Journal ArticleDOI
Promising anti-inflammatory effects of chalcones via inhibition of cyclooxygenase, prostaglandin E2, inducible NO synthase and nuclear factor κb activities.
TL;DR: This review focuses on the anti-inflammatory effects of chalcones, caused by their inhibitory action primarily against the activities and expressions of four key inflammatory mediators viz., cyclooxygenase, prostaglandin E2, inducible NO synthase, and nuclear factor κB.
Journal ArticleDOI
Chalcone Derivatives: Role in Anticancer Therapy
TL;DR: Chalcones (1,3-diaryl-2-propen-1-ones) are precursors for flavonoids and isoflavonoids, which are common simple chemical scaffolds found in many naturally occurring compounds as discussed by the authors.
Journal ArticleDOI
The Keap1/Nrf2-ARE Pathway as a Pharmacological Target for Chalcones
Matheus de Freitas Silva,Letizia Pruccoli,Fabiana Morroni,Giulia Sita,Francesca Seghetti,Claudio Viegas,Andrea Tarozzi +6 more
TL;DR: Anti-inflammatory activity was more evident than others, suggesting a multi-target Michael acceptor mechanism for the chalcones involving key regulators of the Nrf2 and nuclear factor- κB (NF-κB) pathways.
Journal ArticleDOI
A review of ligand-based virtual screening web tools and screening algorithms in large molecular databases in the age of big data
TL;DR: This review discusses a representative set of online virtual screening servers and their underlying similarity algorithms, and the challenges that future works must solve in a virtual screening framework.
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