Synthesis, dimerization, and biological activity of hexaoxygenated chalcones related to calythropsin and combretastatins.
Five new hexaoxygenated chalcones and one new chalcone photodimer were synthesized and their cytotoxicity against leukemia cell line L-1210 was studied. The three more active compounds were tested for their activity on the inhibition and promotion of tubulin assembly and it was found that these chalcones do not interfere with the tubulin-microtubule system at cytotoxic concentrations, and therefore operate by some different mechanism of action.
Seguin
Elisabeth
E
Laboratoire de Pharmacognosie, UFR de Médecine-Pharmacie, Université de Rouen-Haute Normandie, France. skaltsounis@pharm.uoa.gr
Elomri
Abdelhakim
A
Magiatis
Prokopios
P
Skaltsounis
Alexios-Leandros
AL
Chao
Lin Rui
LR
Tillequin
François
F
D000818:Animals; D001921:Brain; D002599:Chalcone / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D020128:Inhibitory Concentration 50; D007938:Leukemia; D051379:Mice; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D010777:Photochemistry / Q000379:methods; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D013552:Swine; D014404:Tubulin / Q000096:biosynthesis / Q000187:drug effects / Q000378:metabolism*; D014407:Tumor Cells, Cultured / Q000187:drug effects
D014404:Tubulin; D002599:Chalcone