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Isobrassinin and its analogues: novel types of antiproliferative agents
Péter Csomós1, István Zupkó, Borbála Réthy
1Institute of Pharmaceutical Chemistry, University of Szeged and Research Group for Heterocyclic Chemistry, Hungarian Academy of Sciences, H-6701, PO Box 427, Hungary.
Abstract:
Isobrassinin (2-(S-methyldithiocarbamoylaminomethyl)indole (7a), a regioisomer of the cruciferous phytoalexin brassinin (1), exerted marked antiproliferative effects on the HeLa, A431 and MCF7 cell lines (>78.6% inhibition at 30muM). For structure-activity relationships, further analogues were synthesized. The highest cytotoxic effect was displayed by 2-phenylimino-1,3-thiazino[5,6-b]indole (10) (10 microM, 76.8%-HeLa and 46.3%-MCF7). The effect of the natural phytoalexin brassinin was also determined.
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