New brefeldin a derivatives and their utility in the...

C - Chemistry – Metallurgy – 07 – D

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C07D 313/00 (2006.01) A61K 31/365 (2006.01) A61K 31/395 (2006.01) C07D 405/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) C07D 419/12 (2006.01)

Patent

CA 2193704

Provided are brefeldin A derivatives of formula (II), wherein one of R1 and R2 is H and the other of R1 and R2 is a substituent group having 1 to 12 carbon atoms containing a basic nitrogen atom or a quaternary ammonium group, or a salt thereof. These derivatives exhibit good antitumor activity, and are administrable to human patients without the problems associated with brefeldin A.

Dérivés de bréfeldine A de formule générale (II) dans laquelle R¿1? ou R¿2? est H et l'autre est un groupe substituant possédant 1 à 12 atomes de carbone et contenant un atome d'azote de base ou un groupe ammonium quaternaire, ou un sel desdits dérivés. Lesdits dérivés présentent une bonne activité antitumorale et peuvent être administrés à des patients humains sans rencontrer les problèmes associés à la bréfeldine A.

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