Design, synthesis and biological evaluation of novel curcumin analogues as anti-neoplastic agents

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

Research output: Contribution to journalArticle

20 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)304-310
Number of pages7
JournalLetters in Drug Design and Discovery
Volume3
Issue number5
DOIs
StatePublished - Jul 10 2006

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Curcumin
Tetralones
Cytostatic Agents
Ketones
Neoplasms
Cell Line
Direction compound
In Vitro Techniques

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery

Cite this

Jha, A., Zhao, J., Cameron, T. S., De Clercq, E., Balzarini, J., Manavathu, E. K., & Stables, J. P. (2006). Design, synthesis and biological evaluation of novel curcumin analogues as anti-neoplastic agents. Letters in Drug Design and Discovery, 3(5), 304-310. https://doi.org/10.2174/157018006777574131

Design, synthesis and biological evaluation of novel curcumin analogues as anti-neoplastic agents. / Jha, Amitabh; Zhao, Jin; Cameron, T. Stanley; De Clercq, Erik; Balzarini, Jan; Manavathu, Elias K.; Stables, James P.

In: Letters in Drug Design and Discovery, Vol. 3, No. 5, 10.07.2006, p. 304-310.

Research output: Contribution to journalArticle

Jha, A, Zhao, J, Cameron, TS, De Clercq, E, Balzarini, J, Manavathu, EK & Stables, JP 2006, 'Design, synthesis and biological evaluation of novel curcumin analogues as anti-neoplastic agents', Letters in Drug Design and Discovery, vol. 3, no. 5, pp. 304-310. https://doi.org/10.2174/157018006777574131
Jha, Amitabh ; Zhao, Jin ; Cameron, T. Stanley ; De Clercq, Erik ; Balzarini, Jan ; Manavathu, Elias K. ; Stables, James P. / Design, synthesis and biological evaluation of novel curcumin analogues as anti-neoplastic agents. In: Letters in Drug Design and Discovery. 2006 ; Vol. 3, No. 5. pp. 304-310.
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