Exploring The Recent Advances In Anti-Cancer Potency Of Chalcone Containing Hybrids

Abstract

Chalcones due to their easy and simple synthesis route and broad spectrum of biological activities, emerged as the outstanding candidate for medicinal and pharmaceutical chemistry. In addition to numerous other biological activities, anticancer activity of the chalcone-based compounds has been in particular focused, and is being predominantly mediated through apoptosis induction, cell cycle arrest, angiogenesis & metastasis inhibition as well as by modulating key signalling pathways which include NF-κB, PI3K/Akt/mTOR, MAPK and STAT3. An outstanding chalcone-based hybrid development has been witnessed in the past decade, explicitly aimed at different human cancer cell lines for potency and selectivity. The bioactivities were remarkably increased when introducing heterocycles, halogen substituents and fusing to other drug-like moieties into the chalcone scaffold. This not only results in enhanced cytotoxicity against cancer cells, but also lower toxicity on benign cell and opens many new drug candidates. There are already a number of chalcone derivatives such as sofalcone and metochalcone, which have been administered clinically for several years. This review provides a detailed account of the developments, from inception to date, in the synthesis and mechanistic study as well as in-vitro assays of chalcone-based hybrids specifically for their potential role as anticancer agents.