127034-22-4Relevant academic research and scientific papers
Combretastatin-like chalcones as inhibitors of microtubule polymerization. Part 1: Synthesis and biological evaluation of antivascular activity
Ducki, Sylvie,Rennison, David,Woo, Meiko,Kendall, Alexander,Chabert, Jeremie Fournier Dit,McGown, Alan T.,Lawrence, Nicholas J.
supporting information; experimental part, p. 7698 - 7710 (2010/03/24)
The α-methyl chalcone SD400 is a potent inhibitor of tubulin assembly and possesses potent anticancer activity. Various chalcone analogues were synthesized and evaluated for their cell growth inhibitory properties against the K562 human chronic myelogenous leukemia cell line (SD400, IC50 0.21 nM; combretastatin A4 CA4, IC50 2.0 nM). Cell cycle analysis by flow cytometry indicated that these agents are antimitotic (SD400, 83% of the cells are in G2/M phase; CA4 90%). They inhibit tubulin assembly at low concentration (SD400, IC50 0.46 μM; CA4, 0.10 μM) and compete with [3H]colchicine for binding to tubulin (8% [3H]colchicine remained bound to tubulin after competition with SD400 or CA4). Upon treatment with SD400, remarkable cell shape changes were elicited in HUVEC cells, consistent with vasculature damaging activity.
Synthesis and inhibitory activity of dimethylamino-chalcone derivatives on the induction of nitric oxide synthase
Rojas, Javier,Domínguez, José N,Charris, Jaime E,Lobo, Gricela,Payá, Miguel,Ferrándiz, M.Luisa
, p. 699 - 705 (2007/10/03)
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
Novel use of compounds of the chalcones class
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, (2008/06/13)
Process for inhibiting vascularization of a tumor mass comprising administering, in an amount effective to inhibit vascularization, at least one chalcone of formula (I): wherein: R is chosen from a hydrogen atom, a methyl group, an ethyl group, a chlorine atom, and a bromine atom, A is an NR1R2 group, wherein R1 and R2, which may be identical or different, are each chosen from a methyl group and an ethyl group, and n is an integer equal to 2 or 3.
Potent antimitotic and cell growth inhibitory properties of substituted chalcones
Ducki, Sylvie,Forrest, Richard,Hadfield, John A.,Kendall, Alex,Lawrence, Nicholas J.,McGown, Alan T.,Rennison, David
, p. 1051 - 1056 (2007/10/03)
A series of substituted chalcones was synthesised and screened for cytotoxic activity against the K562 human leukaemia cell line. (E)-3-(3'- Hydroxy-4'-methoxyphenyl)-2-methyl-1-(3',4',5'-trimethoxyphenyl)-prop-2-en- 1-one [IC50 (K562) 0.21 nM] was found to be the most active. A relationship between the conformation and cytotoxicity of the chalcones is discussed.
Chalcones: A new class of antimitotic agents
Edwards,Stemerick,Sunkara
, p. 1948 - 1954 (2007/10/02)
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
