2-arylbenzazole compounds

Details 2-arylbenzazole compounds 2-arylbenzazole compounds

C - Chemistry, Metallurgy

07

D

C07D 277/66 (2006.01) A61K 31/42 (2006.01) A61K 31/425 (2006.01) C07D 263/57 (2006.01)

Patent

CA 2213737

There are disclosed herein 2-phenylbenzazole compounds having a 3'-substituent and a 4'-NR5R6 substituent in the phenyl group where R5 and R6 are each hydrogen or alkyl, or where the 4'-NR5R6 substituent is N-acyl (or N-benzoyl). There are also disclosed 2-phenylbenzazole compounds in the form of 4'-N sulphamate salts. Such compounds exhibit significant selective cytotoxic activity in respect of tumor cells and provide potentially useful chemotherapeutic agents for selective treatment of a range of cancers. The compounds have the general formula I: (see formula I)

Cette invention concerne des composés 2-phénylbenzazole ayant un substituant en 3' et un substituant NR<5>R<6> en 4' dans le groupe phényle, R<5> et R<6> étant chacun l'hydrogène ou un alkyle, ou le substituant NR<5>R<6> en 4' étant un N-acyle (ou un N-benzoyle). L'invention se rapporte également à des composés 2-phényl-benzazole sous la forme de sels de sulphamate portant N en 4'. De tels composés présentent une activité cytotoxique sélective significative vis-à-vis des cellules tumorales et permettent de disposer d'agents chimiothérapeutiques potentiellement utiles pour le traitement sélectif d'un certain nombre de cancers.

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