Privileged structures have been widely used as an effective template in medicinal chemistry for drug discovery. Chalcone is a common simple scaffold found in many naturally occurring compounds. Many chalcone derivatives have also been prepared due to their convenient synthesis. These natural products and synthetic compounds have shown numerous interesting biological activities with clinical potentials against various diseases. This review aims to highlight the recent evidence of chalcone as a privileged scaffold in medicinal chemistry. Multiple aspects of chalcone will be summarized herein, including the isolation of novel chalcone derivatives, the development of new synthetic methodologies, the evaluation of their biological properties, and the exploration of the mechanisms of action as well as target identification. This review is expected to be a comprehensive, authoritative, and critical review of the chalcone template to the chemistry community.

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Chalcone: A Privileged Structure in Medicinal Chemistry.

Chalcone scaffolds as anti-infective agents: Structural and molecular target perspectives

Chalcone is an aromatic ketone that forms the central core of many important biological compounds, which are known as chalcones. Chalcones are the biogenetic precursors of flavonoids and isoflavonoids, which are abundant in plants. Chalcones are active lead molecules in medicinal chemistry for the discovery of new drugs. Here, we review properties, biosynthesis and structural diversity of natural chalcones. Then, we present the synthesis of chalcones and their biological activities with focus on structure–activity relationships. Pharmaceutically important and patented chalcones are also discussed.

Chalcone synthesis, properties and medicinal applications: a review

L-Proline catalysed multicomponent synthesis of 3-amino alkylated indolesvia a Mannich-type reaction under solvent-free conditions

Introduction: Chalcones are one of the major classes of naturally occurring compounds. A large number of synthetic routes have been reported for the synthesis of chalcones, the most classical and general being the Claisen–Schmidt condensation. Chalcones and their derivatives have a huge importance in medicinal chemistry, displaying a wide range of important pharmacological activities.Areas covered: The authors provide an overview of the recent scientific reports describing the obtention and study of new chalcones. The review emphasizes the rationale behind the natural sources, the discovery, the design, the synthesis, the biological activities and the study of structure–activity relationships of the new chalcone derivatives. The article is based on the literature published from June 2011 – 2014 related to the development of this family of compounds. The patents presented in this review have been collected from multiple electronic databases including Scifinder, Espacenet and Mendeley.Expert opinion: Althou...

Potential pharmacological uses of chalcones: a patent review (from June 2011 – 2014)

https://www.rsc.org/suppdata/GC/C0/C0GC00523A/C0GC00523A.PDF

β-Cyclodextrin catalysed synthesis of tryptanthrin in water

Synthesis of chalcones and flavanones using Julia–Kocienski olefination

Design and synthesis of 1,3-biarylsulfanyl derivatives as new anti-breast cancer agents.

An efficient new multicomponent protocol for the C-3 functionalization of indoles with dihydrocoumarin has been developed using an artificial sweetener (saccharin)-based functional ionic liquid (imidazolium saccharinate). The reaction consists of the Knoevenagel coupling of salicylaldehyde and Meldrum's acid followed by a Michael type reaction with indole, resulting in concomitant lactonization via decarboxylative elimination to yield indole-3-dihydro-coumarins in good to excellent yields at room temperature.

A novel access to indole-3-substituted dihydrocoumarins in artificial sweetener saccharin based functional ionic liquids

Arylethanones of type (I) and (IV) are applied as Julia coupling partners for the reaction with aromatic aldehydes to give chalcones and flavanones, correspondingly.

Vishwa Deepak Tripathi

Papers

β-Cyclodextrin catalysed synthesis of tryptanthrin in water

Synthesis of chalcones and flavanones using Julia–Kocienski olefination

Design and synthesis of 1,3-biarylsulfanyl derivatives as new anti-breast cancer agents.

A novel access to indole-3-substituted dihydrocoumarins in artificial sweetener saccharin based functional ionic liquids

Synthesis of Chalcones and Flavanones Using Julia—Kocienski Olefination.