Chalcones belong to the flavonoid class of phenolic compounds. They form one of the largest groups of bioactive natural products. The potential anticancer, anti-inflammatory, antimicrobial, antioxidant, and antiparasitic properties of naturally occurring chalcones, and their unique chemical structural features inspired the synthesis of numerous chalcone derivatives. In fact, structural features of chalcones are easy to construct from simple aromatic compounds, and it is convenient to perform structural modifications to generate functionalized chalcone derivatives. Many of these synthetic analogs were shown to possess similar bioactivities as their natural counterparts, but often with an enhanced potency and reduced toxicity. This review article aims to demonstrate how bioinspired synthesis of chalcone derivatives can potentially introduce a new chemical space for exploitation for new drug discovery, justifying the title of this article. However, the focus remains on critical appraisal of synthesized chalcones and their derivatives for their bioactivities, linking to their interactions at the biomolecular level where appropriate, and revealing their possible mechanisms of action.

Centre for Natural Products Discovery School of Pharmacy and Biomolecular Sciences Liverpool John Moores University James Parsons Building Byrom Street Liverpool L3 3AF UK

Department of Biology College of Education for Pure Sciences University of Anbar Al Anbar 10081 Iraq

Department of Biology College of Education for Women University of Anbar Al Anbar 10081 Iraq

Faculty of Science and Engineering University of Wolverhampton Wolverhampton WV1 1LY UK

Laboratory of Growth Regulators Institute of Experimental Botany ASCR and Palacký University Šlechtitelů 27 78371 Olomouc Czech Republic

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