- Synthesis and inhibitory activity of dimethylamino-chalcone derivatives on the induction of nitric oxide synthase
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A series of nine dimethylamino-chalcone derivatives (1,3-diaryl-propenones) was synthesized and screened as potential inhibitors of NO and PGE2 production in the RAW 264.7 macrophage cell line. 4-Dimethylamino-2′,5′-dimethoxychalcone (6) was fo
- Rojas, Javier,Domínguez, José N,Charris, Jaime E,Lobo, Gricela,Payá, Miguel,Ferrándiz, M.Luisa
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p. 699 - 705
(2007/10/03)
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- Antimalarial alkoxylated and hydroxylated chalones: Structure-activity relationship analysis
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Chalcones with 2′,3′,4′-trimethoxy, 2′,4′-dimethoxy, 4′-methoxy, 4′-ethoxy, 2′,4′-dihydroxy, and 4′-hydroxy groups on ring B were synthesized and evaluated in vitro against Plasmodium falciparum (K1) in a [3H] hypoxanthine uptake assay. The other ring A was quinoline, pyridine, naphthalene, or phenyl rings with electron-donating or electron-withdrawing substituents of varying lipophilicities. Trimethoxy 6 and 27, dimethoxy 7, 8, 29, and methoxy 31 analogues had good in vitro activities (IC50 5μM). 3-Quinolinyl ring A derivatives were well represented among the active compounds. Hydroxylated chalcones were less active than the corresponding alkoxylated analogues. When evaluated in vivo, 8 and 208 were comparable to chloroquine in extending the lifespan of infected mice. Multivariate data analysis showed that in vitro activity was mainly determined by the properties of ring B. Quantitative structure - activity relationship models with satisfactory predictive ability were obtained for various B ring chalcones using projections to latent structures. A model with good predictability was proposed for 19 active chalcones. Size and hydrophobicity were identified as critical parameters.
- Liu,Wilairat,Go
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p. 4443 - 4452
(2007/10/03)
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- Chalcones: A new class of antimitotic agents
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A series of chalcones was evaluated as antimitotic agents. One of these, (E)-1-(2,5-dimethoxyphenyl)-3-[4-(dimethylamino)phenyl]-2-methyl-2-propen- 1-one) (73), was found to be an effective antimitotic agent at a concentration of 4 nM in an in vitro HeLa
- Edwards,Stemerick,Sunkara
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p. 1948 - 1954
(2007/10/02)
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