Synthesis and differential antiproliferative activity of Biginelli compounds against cancer cell lines: Monastrol, oxo-monastrol and oxygenated analogues |
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Authors: | Russowsky Dennis Canto Rômulo F S Sanches Sergio A A D'Oca Marcelo G M de Fátima Angelo Pilli Ronaldo A Kohn Luciana K Antônio Márcia A de Carvalho João Ernesto |
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Institution: | Instituto de Química, Universidade Federal do Rio Grande do Sul, CP 15003, 91501-970 Porto Alegre, RS, Brazil. dennis@iq.ufrgs.br |
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Abstract: | The synthesis and differential antiproliferative activity of monastrol (1a), oxo-monastrol (1b) and eight oxygenated derivatives 3a,b-6a,b on seven human cancer cell lines are described. For all evaluated cell lines, monastrol (1a) was shown to be more active than its oxo-analogue, except for HT-29 cell line, suggesting the importance of the sulfur atom for the antiproliferative activity. Monastrol (1a) and the thio-derivatives 3a, 4a and 6a displayed relevant antiproliferative properties with 3,4-methylenedioxy derivative 6a being approximately more than 30 times more potent than monastrol (1a) against colon cancer (HT-29) cell line. |
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Keywords: | Monastrol Dihydropyrimidinones Antiproliferative Cancer Mitotic kinesin Eg5 |
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