Isobrassinin and its analogues: Novel types of antiproliferative agents

P Csomós, I Zupkó, B Réthy, L Fodor, G Falkay…

Index: Csomos, Peter; Zupko, Istvan; Rethy, Borbala; Fodor, Lajos; Falkay, George; Bernath, Gabor Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 24 p. 6273 - 6276

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Citation Number: 28

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 30μM). 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)(10μM, 76.8%—HeLa and 46.3%—MCF7). ...