Abstract |
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.
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Authors | Jin Tatsuzaki, Kenneth F Bastow, Kyoko Nakagawa-Goto, Seiko Nakamura, Hideji Itokawa, Kuo-Hsiung Lee |
Journal | Journal of natural products
(J Nat Prod)
Vol. 69
Issue 10
Pg. 1445-9
(Oct 2006)
ISSN: 0163-3864 [Print] United States |
PMID | 17067159
(Publication Type: Journal Article, Research Support, N.I.H., Extramural)
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Chemical References |
- ATP Binding Cassette Transporter, Subfamily B, Member 1
- Antineoplastic Agents
- Chalcones
- Styrenes
- Eugenol
- isoeugenol
- methyl-3-methoxy-4-hydroxystyryl ketone
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Topics |
- ATP Binding Cassette Transporter, Subfamily B, Member 1
(physiology)
- 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
- Styrenes
(chemical synthesis, chemistry, pharmacology)
- Tumor Cells, Cultured
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