Chalcones: a new class of antimitotic agents

Abstract

A series of chalcones was evaluated as antimitotic agents. One of these, (E)-1-(2,5-dimethoxyphenyl)-3-[4-(dimethylamino)phenyl]-2-methyl-2-pr open- 1-one) (73), was found to be an effective antimitotic agent at a concentration of 4 nM in an in vitro HeLa cell test system. When evaluated in experimental tumor models in vivo, this compound exhibited antitumor activity against L1210 leukemia and B16 melanoma.

Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents

“…These compounds were 7 chosen on the basis of structural similarity to 1 (all with the exception of colchicine contain a linear double bond linking two ring systems, one of which is substituted with 2 or more methoxy groups), antiproliferative potency, and tubulin-targeting activity. These chalcones were synthesised and characterised by published procedures (compound 14 [8], 15 [20], 16 [8], 17 [21]). …”

Biotransformation of chalcones by the endophytic fungus Aspergillus flavus isolated from Paspalum maritimum trin

“…The chalcones 1 (68.5% yield), 27 2 (75.0% yield) 28 and 3 (60.0% yield) 29 were synthesized using methodology described in the literature 18 and their structures were determined by the analysis of 1D-and 2D-NMR, mass spectral information and comparison with reported physical and spectroscopic data. These chalcones were bioreduced by Aspergillus flavus producing the dihydrochalcones 4 (74.5% yield), 5 (36.3% yield) and 6 (15.6% yield), respectively, after 10 days of reaction ( Figure 1).…”

Microwave-Assisted Synthesis and Cytotoxicity Evaluation of Some Novel Pyrazole Containing Imidiazole, Pyrazole, Oxazole, Thiadiazole and Benzochromene derivatives

“…Applying the typical procedure of Claisene Schmidt condensation for the synthesis of chalcones [36] from 3-methyl-1-phenyl-1H-pyrazole-4-carboxaldehyde (1) and acetophenone (2a) or 2-acetyl-thiophene (2b) as our model reaction. Initially, the stirring of an equimolar mixture of both compounds in ethanol, at ambient temperature, in the presence of 10 % aq.…”