Podophyllotoxins as antiproliferative agents

Details Podophyllotoxins as antiproliferative agents Podophyllotoxins as antiproliferative agents

C - Chemistry, Metallurgy

07

D

C07D 493/04 (2006.01) A61K 31/34 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2468479

The invention relates to podophyllotoxins, uses thereof and methods of their production. In order to create hydrolytically activated prodrugs of etoposide VP-16 as inactive precursor molecules which are activated by hydrolysis, derivatives of the 4' phenolic hydroxy group were synthesised. The prodrugs of the present invention are stable under a wide range of pH values, yet can be activated by an appropriate change of pH, as well as under physiological conditions in the presence of naturally occurring enzymes. The prodrugs of the present invention reduce adverse reactions when administered to a patient and are capable of overcoming multidrug resistance commonly encountered with the parent molecule.

L'invention concerne des podophyllotoxines, des utilisations de celles-ci ainsi que des procédés de production de celles-ci.

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