Synthesis and biotests of 2-aryl-5-arylmethylidene-substituted 1,3-oxazol-5(4H)-ones and N-methyl-3,5-dihydro-4H-imidazol-4-ones as combretastatin A-4 analogs |
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| Authors: | E. S. Barskaia A. A. Beloglazkina B. Wobith N. A. Zefirov A. G. Majouga E. K. Beloglazkina N. V. Zyk S. A. Kuznetsov O. N. Zefirova |
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| Affiliation: | 1.Department of Chemistry,M. V. Lomonosov Moscow State University,Moscow,Russian Federation;2.Institute of Biological Sciences,University of Rostock,Rostock,Germany;3.Institute of Physiologically Active Compounds,Russian Academy of Sciences,Chernogolovka,Russian Federation |
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| Abstract: | A series of 2-aryl-5-arylmethylidene-1,3-oxazol-5(4H)-ones and 2-aryl-5-arylmethylidene-N-methyl-3,5-dihydro-4H-imidazol-4-ones was synthesized as structural analogs of combret- astatin A-4 (a compound possessing antitumor activity). (5Z)-5-[(4-Methoxyphenyl)methyl-idene]-3-methyl-2-(4-methylphenyl)-3,5-dihydro-4H-imidazol-4-one was found to exhibit the highest cytotoxicity against cells of human A549 lung carcinoma line (EC50 = 6±0.8 μmol L?1). |
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