Advances in Chalcones with Anticancer Activities
Chandrabose Karthikeyan, Narayana S.H. Narayana Moorthy, Sakthivel Ramasamy, Uma Vanam, Elangovan Manivannan, Devarajan Karunagaran and Piyush Trivedi
Affiliation: School of Pharmaceutical Sciences, Rajiv Gandhi Proudyogiki Vishwavidyalaya, Airport Bypass Road, Gandhi Nagar, Bhopal, MP, 462036, India.
Keywords: Anticancer, anticancer chalcones, antioxidant, antiproliferative activity, chalcones, patents.
Chalcones are naturally occurring compounds exhibiting broad spectrum biological activities including anticancer
activity through multiple mechanisms. Literature on anticancer chalcones highlights the employment of three pronged strategies,
namely; structural manipulation of both aryl rings, replacement of aryl rings with heteroaryl scaffolds, molecular hybridization
through conjugation with other pharmacologically interesting scaffolds for enhancement of anticancer properties.
Methoxy substitutions on both the aryl rings (A and B) of the chalcones, depending upon their positions in the aryl rings appear
to influence anticancer and other activities. Similarly, heterocyclic rings either as ring A or B in chalcones, also influence
the anticancer activity shown by this class of compounds. Hybrid chalcones formulated by chemically linking chalcones to
other prominent anticancer scaffolds such as pyrrol[2,1-c][1,4]benzodiazepines, benzothiazoles, imidazolones have demonstrated
synergistic or additive pharmacological activities. The successful application of these three pronged strategies for discovering
novel anticancer agents based on chalcone scaffold has resulted in many novel and chemically diverse chalcones
with potential therapeutic application for many types of cancer. This review summarizes the concerted efforts expended on
the design and development of anticancer chalcones recorded in recent literature and also provides an overview of the patents
published in this area between 2007 and 2014 (WO2013022951, WO201201745 & US2012029489).
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