Synthesis and evaluation of a series of novel imidazolidinone analogues of 6-aminoflavone as anticancer and anti-inflammatory agents

Moorkoth, Sudheer and Srinivasan, KK and Kutty, Gopalan N and Alex, Joseph and Naseer, M (2012) Synthesis and evaluation of a series of novel imidazolidinone analogues of 6-aminoflavone as anticancer and anti-inflammatory agents. Medicinal Chemistry Research, 22 (3). pp. 1-12. ISSN DOI 10.1007/s00044-013-0486-7

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Abstract

The flavone moiety is a potential pharmacophore known for its diverse range of pharmacological activities. Aminoflavones have recently been the subject of considerable attention as lead molecules in several cancer research projects. Imidazolidinone heterocycles represent another biologically active scaffold with known cytotoxic properties. In an attempt to provide synergistic cytotoxic activity, these two moieties have been combined, and the resulting novel analogues evaluated for their anticancer and anti-inflammatory activities. The results revealed that the cytotoxicities of these compounds were fivefold greater than those of aminoflavone. DNA histograms obtained from cell cycle analysis in the presence of these compounds were apoptotic in their nature. Furthermore, the in vivo screening of these compounds using Ehrlich’s ascites tumour model showed an increase in life span, whereas an in vivo anti-inflammatory study resulted in the enhancement of the anti-inflammatory potential. The results therefore supported the hypothesis that there is a relationship between inflammation and cancer

Item Type: Article
Uncontrolled Keywords: 6-Aminoflavone;Imidazolidinone; Cytotoxicity; Ehrlich’s ascites; Anti-inflammatory;Carrageenan
Subjects: Pharmacy > MCOPS Manipal > Pharmaceutical Chemistry
Pharmacy > MCOPS Manipal > Pharmaceutical Quality Assurance
Pharmacy > MCOPS Manipal > Pharmacology
Depositing User: KMC Manipal
Date Deposited: 15 Feb 2013 10:11
Last Modified: 15 Feb 2013 10:11
URI: http://eprints.manipal.edu/id/eprint/78441

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