In vitro biological activities of new heterocyclic chalcone derivatives
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Med Chem Res (2013) 22:2079–2087 DOI 10.1007/s00044-012-0193-9
ORIGINAL RESEARCH
In vitro biological activities of new heterocyclic chalcone derivatives Chenna Govindaraju Darshan Raj • Balladaka Kunchanna Sarojini • Subramanya Hegde • Swamy Sreenivasa • Yalega Siddappa Ravikumar • Veerakyathappa Bhanuprakash • Yogisharadhya Revanaiah • Ramappa Ragavendra
Received: 21 March 2012 / Accepted: 6 August 2012 / Published online: 18 September 2012 Ó Springer Science+Business Media, LLC 2012
Abstract This work reports the synthesis and characterization of new heterocyclic chalcone derivatives 3(a–j) and in vitro biological evaluation for antiproliferative, antioxidant, antibacterial, antifungal, and antiviral properties. The antiproliferative efficacy and LC50 of the compounds against HepG2 cell lines were determined. The LC50 for 3d was found to be 8 lg/mL. All the compounds exhibited moderate DPPH scavenging activity and moderate to good antimicrobial activity against tested bacterial and fungal strains. Further, the compounds at their respective maximum non-toxic concentrations did not inhibit DNA viruses like buffalopox, camelpox, and goatpox.
C. G. D. Raj B. K. Sarojini (&) Department of Chemistry, P.A. College of Engineering, Nadupadavu, Mangalore 574153, Karnataka, India e-mail: [email protected]; [email protected] S. Hegde S. Sreenivasa Department of P.G. Studies and Research in Chemistry, University College of Science, Tumkur University, Tumkur 572101, Karnataka, India Y. S. Ravikumar Department of Biotechnology, M.S. Ramaiah Institute of Technology, Bangalore 5600054, Karnataka, India V. Bhanuprakash Y. Revanaiah Division of Virology, Indian Veterinary Research Institute, Mukteswar 263138, Uttaranchal, India R. Ragavendra Department of P.G. Studies and Research Biochemistry, Kuvempu University, Jnana Sahyadri, Shankaraghatta 577451, Karnataka, India
Keywords Novel heterocyclic chalcone derivatives Antioxidant activity Antimicrobial property Antiviral studies
Introduction The great upsurge in the research of organic chemistry worldwide during the past few decades has contributed enormously to the growth of pharmaceuticals. The importance of heterocyclic compounds in the area of medicine is well known, and they amount to one-third of the known organic compounds. Compounds with a heterocyclic ring are inextricably woven into most basic bio-chemical processes of life. With the discovery of highly potent antiinfectious agents, there has been a profound change in medical practice. Otherwise, infections would have taken a major toll on life. Indole, furan, and thiophen nuclei are found to be the main constituents of many natural products and drugs. Methoxylated chalcones were found to be antimitotic against HeLa cells (Echeverria et al., 2009). Synthetic chalcones are inhibitory to human rhinoviruses and plant viruses. Similarly, chalcone and 4,6-dichloroflavan (DCF) interfere with virion uncoating resulting in the inhibition of virus infection. Their variable antiviral activity depends on specific
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