An updated patent review of therapeutic applications of chalcone derivatives (2014-present)

ABSTRACT

Introduction: Chalcone or benzylideneacetophenone or 1,3-diphenyl-2-propene-1-one is a natural product comprising of two aromatic rings connected together by a three-carbon α, β unsaturated carbonyl bridge. It is one of the most privileged scaffolds in medicinal chemistry that can be synthesized in the laboratory and can be converted into several therapeutically active heterocyclic scaffolds. It exhibits multifarious pharmacological activities and also plays a key role in several non-pharmacological scientific applications.

Areas covered: The present article comprehensively focuses on the approved patents during the time duration 2014–2018 on various chalcone molecules with diverse pharmacological activities.

Expert opinion: The study puts forward the latest updated therapeutic applications of chalcone-based compounds as antiproliferative, antidiabetic, anti-infective, anti-inflammatory, antioxidant, antiaging, neuroprotective, and cardioprotective agents. The type, position, and the number of substituents present on the chalcone scaffold have been perceived to play an imperative function in interacting with molecular targets (receptor, enzyme, and/or channel) to express the biological responses. In the majority of the studies, the overall activity of the ligand administered as pharmaceutically acceptable salt is found to be better than that of standard marketed drug preparation. The article will certainly attract (medicinal)-chemists actively involved in the development of therapeutically active scaffolds.

KEYWORDS:

• Chalcone
• patent
• therapeutic
• molecular target
• inhibitor
• anti-cancer
• heterocyclic
• scaffold

Article highlights

• Patent approved or filed on chalcones in the duration of 2014–2018.

• Therapeutic activity of (hetero)aryl substituted chalcone derivatives/analogs.

• Anti-cancer, anti-oxidant, anti-diabetic, anti-infective, anti-inflammatory, anti-aging activities of chalcone.

• Neuroprotective and cardioprotective activities of some recently patented chalcones.

Expert opinion, latest trends, and future prospects of medicinally privileged chalcone based compounds.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This paper has not been funded.