Recent developments in biological aspects of chalcones: the odyssey continues

ABSTRACT

Introduction: Chalcones are attractive to synthetic chemists because they are easy to prepare, have a large number of replaceable hydrogens, thereby having significant biological potential. Chalcones and their derivatives (carbocyclic as well as heterocyclic) exhibit a range of biological properties including anticancer, antimalarial, antioxidant, anti-inflammatory and anti-tubercular activities. Their promising biological profile, along with their ease of synthetic manipulations, have triggered the design and development of new chalcone derivatives as well as their conjugates with active pharmacophores affording therapeutic templates targeting various diseases.

Areas covered: This review focuses on synthesized substituted chalcones as well as chalcone-based molecular conjugates that have been developed between 2015 and 2018. Furthermore, their structure–activity relationships with an emphasis on their mechanism of action and docking studies along with their future therapeutic applications.

Expert opinion: A recent upsurge in scientific literature encompassing the synthesis of new chalcone-derivatives as well as its role in ameliorating the activity profiles via amalgamation with other pharmacophores has clearly established the importance of chalcones in present-day drug discovery. As a point, we, the authors, believe that new effective scaffolds can be developed from chalcones with an added advantage of being available at a low cost.

KEYWORDS:

• Claisen-schmidt condensation
• chalcones
• Structutre Activity Relationship (SAR)
• anti-proliferatives
• anti-oxidant
• anti-malarial

Article highlights

• Chalcones or the α, β-unsaturated ketones, are open chain flavonoids that act as biogenetic precursors of flavonoids in higher plants.

• Claisen-Schmidt condensation is mainly employed for affording chalcones.

• The unique α,β-unsaturated ketone core of chalcone is responsible for the broad-spectrum of biological activities exhibited by this molecule.

• Chalcones and its derivatives have received considerable attention due to their anticancer, antibacterial, antifungal, antimalarial, antioxidant, anti-inflammatory and antitubercular activities.

• Anticancer activity of chalcones could be attributed via induction of apoptosis, blockage cell cycle progression in the G2/M phase and inhibition of tubulin polymerization.

• Chalcones have also exhibited promising antimalarial potential because of their ability to inhibit cysteine/aspartic proteases.

This box summarizes key points contained in the article.

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

The authors are funded by the Council of Scientific and Industrial Research via a Junior Research Fellowship (Reference No. 09/254(0269)/2017-EMR-1) provided to A Rani.