摘要 |
A texaphyrin as shown in formula I, wherein, R1-R4 and R6-R9 are independently hydrogen, halide other than iodide, hydroxyl, alkyl, aryl, haloalkyl other than iodoalkyl, nitro, formyl, acyl, hydroxyalkyl, oxyalkyl, oxyhydroxyalkyl, saccharide, carboxy, carboxyalkyl, carboxyamidealkyl, a site-directing molecule or a couple to a site-directing molecule, R5 and R10 are independently hydrogen, alkyl, aryl, hydroxyalkyl, oxyalkyl, oxyhydroxyalkyl, carboxyalkyl, carboxyamidealkyl or a couple to a site-directing molecule, R11 is alkyl, alkenyl, oxyalkyl or hydroxyalkyl having up to about 3 carbon atoms and having rotational flexibility around a first-bound carbon atom, where R6 and R9 are other than hydrogen, then R5 and R10 are hydrogen or methyl, and where R5 and R10 are other than hydrogen, then R6 and R9 are hydrogen, hydroxyl or halide other than iodide. Also described is a texaphyrin as shown in formula II, wherein, M is H, a divalent metal cation or a trivalent cation, R1-R4 and R6 and R9 are independently hydrogen, halide other than iodide, hydroxyl, alkyl, aryl, haloalkyl other than iodoalkyl, nitro, formyl, acyl, hydroxyalkyl, oxyalkyl, hydroxyalkoxy, saccharide, carboxy, carboxyalkyl, carboxyamidealkyl, a site-directing molecule or a couple to a site-directing molecule, R7 and R8 are independently hydrogen or hydroxyalkoxy, R5 and R10 are independently hydrogen, alkyl, aryl, hydroxyalkyl, oxyalkyl, hydroxyalkoxy, carboxyalkyl, carboxyamidealkyl or a couple to a site-directing molecule, and R11 is alkyl, alkenyl, oxyalkyl or hydroxyalkyl having up to about 3 carbon atoms and having rotational flexibility around a first-bound carbon atom, provided that R6 and R9 are other than hydrogen, then R5 and R10 are hydrogen or methyl, and where R5 and R10 are other than hydrogen, then R6 and R9 are hydrogen, hydroxyl or halide other than iodide, and further provided that at least one of R7 and R8 is hydroxyalkoxy. These compounds are useful as radiation sensitizers.
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