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Recent Patents on Anti-Cancer Drug Discovery
ISSN (Print): 1574-8928
ISSN (Online): 2212-3970
Epub Abstract Ahead of Print
DOI: 10.2174/1574892809666140819153902      Price:  $140









Advances in Chalcones with Anticancer Activities

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Author(s): Chandrabose Karthikeyan, Narayana S. H. Narayana Moorthy, Sakthivel Ramasamy, Uma Vanam, Elangovan Manivannan, Devarajan Karunagaran and Piyush Trivedi
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Abstract:
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 strategy 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 to 2013 (WO2013022951, WO201201745, US2012029489)
Affiliation:
School of Pharmaceutical Sciences, Rajiv Gandhi Proudyogiki Vishwavidyalaya, Airport Bypass Road, Gandhi Nagar, Bhopal, MP, 462036, India