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

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

Volume: 3 Issue: 5

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Jha Amitabh, Zhao Jin, Stanley Cameron T., De Clercq Erik, Balzarini Jan, Manavathu K. Elias and Stables P. James, Design, Synthesis and Biological Evaluation of Novel Curcumin Analogues as Anti-Neoplastic Agents, Letters in Drug Design & Discovery 2006; 3 (5) . https://dx.doi.org/10.2174/157018006777574131