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Isobrassinin and its analogues: novel types of antiproliferative agents |
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| Authors: | Csomós Péter Zupkó István Réthy Borbála Fodor Lajos Falkay George Bernáth Gábor |
| Institution: | aInstitute of Pharmaceutical Chemistry, University of Szeged and Research Group for Heterocyclic Chemistry, Hungarian Academy of Sciences, H-6701, PO Box 427, Hungary bCentral Laboratory, County Hospital, H-5701 Gyula, PO Box 46, Hungary cDepartment of Pharmacodynamics and Biopharmacy, University of Szeged, 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 30 μM). For structure–activity relationships, further analogues were synthesized. The highest cytotoxic effect was displayed by 2-phenylimino-1,3-thiazino5,6-b]indole (10) (10 μM, 76.8%—HeLa and 46.3%—MCF7). The effect of the natural phytoalexin brassinin was also determined. |
| Keywords: | 2-Aminomethylindole Dithiocarbamate Thiazino[5 6-b]indole Antitumour activity |
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