Design, Synthesis and Biological Evaluation of Novel Curcumin Analogues as Anti-Neoplastic Agents

Author(s): Amitabh Jha , Jin Zhao , T. Stanley Cameron , Erik De Clercq , Jan Balzarini , Elias K. Manavathu , James P. Stables .

Journal Name: Letters in Drug Design & Discovery

Volume 3 , Issue 5 , 2006

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A series of novel curcumin analogues were synthesized and bioevaluated for anti-neoplastic activity. These compounds are 2-tetralone-based unsymmetrical α, β-unsaturated ketones with extended conjugation. The majority of the analogues were found to show moderate anti-cancer activity in in-vitro test systems against representative murine and human cancer cell lines. Evidence was obtained that these compounds display cytostatic activity against certain malignant cells and were well tolerated in mice. This study has also revealed various directions whereby the project may be augmented in the future with a view to finding compounds with increased cytotoxicity to neoplastic cells.

Keywords: Molecular Modeling, X-Ray Crystallography, Cytostatic, Antifungal, electrophilic effect

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Article Details

Year: 2006
Page: [304 - 310]
Pages: 7
DOI: 10.2174/157018006777574131
Price: $58

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