Dehydrozingerone, chalcone, and isoeugenol analogues as in vitro anticancer agents.

Twenty-eight compounds related to dehydrozingerone (1), isoeugenol (3), and 2-hydroxychalcone (4) were synthesized and evaluated in vitro against human tumor cell replication. Except for isoeugenol analogues 27-35, most compounds exhibited moderate or strong cytotoxic activity against KB, KB-VCR (a multidrug-resistant derivative), and A549 cell lines. In particular, chalcone 15 showed significant cytotoxic activity against the A549 cell line with an IC50 value of 0.6 microg/mL. Furthermore, dehydrozingerone analogue 11 and chalcones 16 and 17 showed significant and similar cytotoxic activity against both KB (IC50 values of 2.0, 1.0, and 2.0 microg/mL, respectively) and KB-VCR (IC50 values of 1.9, 1.0, and 2.0 microg/mL, respectively) cells, suggesting that they are not substrates for the P-glycoprotein drug efflux pump.
AuthorsJin Tatsuzaki, Kenneth F Bastow, Kyoko Nakagawa-Goto, Seiko Nakamura, Hideji Itokawa, Kuo-Hsiung Lee
JournalJournal of natural products (J Nat Prod) Vol. 69 Issue 10 Pg. 1445-9 (Oct 2006) ISSN: 0163-3864 [Print] United States
PMID17067159 (Publication Type: Journal Article, Research Support, N.I.H., Extramural)
Chemical References
  • Antineoplastic Agents
  • Chalcones
  • P-Glycoprotein
  • Styrenes
  • Eugenol
  • methyl-3-methoxy-4-hydroxystyryl ketone
  • isoeugenol
  • Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
  • Chalcones (chemical synthesis, chemistry, pharmacology)
  • Drug Resistance, Multiple
  • Drug Resistance, Neoplasm
  • Drug Screening Assays, Antitumor
  • Eugenol (analogs & derivatives, chemical synthesis, chemistry, pharmacology)
  • Humans
  • Inhibitory Concentration 50
  • Molecular Structure
  • P-Glycoprotein (physiology)
  • Styrenes (chemical synthesis, chemistry, pharmacology)
  • Tumor Cells, Cultured

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research network!

Choose Username:
Verify Password: