Bioreductive cytotoxic agents
AssigneeShiongi BioResearch Corp.
InventorsMitsunori Ono, Keizo Koya, Lijun Sun, Yumiko Wada, Wojciech Wrona, Natalie Dales, Xueliang Tao, Sylvia Holden
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Abstract
A compound which consists of a proactive alkylating moiety containing an electron-withdrawing group, a bioreductive moiety containing at least two double bonds, and a linker joining the proactive alkylating moiety and the bioreductive moiety.
Claims21
A compound consisting of a proactive alkylating moiety containing an electron-withdrawing group, a bioreductive moiety containing at least two double bonds, and a linker joining the proactive alkylating moiety and the bioreductive moiety, wherein the linker is a methylene group, a C.sub.3 hydrocarbon chain containing a double bond, or a C.sub.5 hydrocarbon chain containing two alternate double bonds;
- the double bonds of the bioreductive moiety, either by themselves when the linker is a methylene group, or together with the double bond of the C.sub.3 linker or the double bonds of the C.sub.5 linker, form a conjugated system, which allows electrons to flow from the bioreductive moiety to the electron-withdrawing group of the proactive alkylating moiety upon reduction of the bioreductive moiety, thereby breaking the bond between the electron-withdrawing group and the linker and converting the proactive alkylating moiety into an active alkylating compound;
- or a salt thereof.
Dependencies are inferred from the claim text.