초록 ▼

Texaphyrins are provided for use as radiation sensitizers. Advantageous properties of texaphyrins for use as a radiation sensitizer include: i) a low redox potential which allows radiation-induced hydrated electrons to flow to texaphyrin rather than neutralizing hydroxyl radicals, allowing hydroxyl

Texaphyrins are provided for use as radiation sensitizers. Advantageous properties of texaphyrins for use as a radiation sensitizer include: i) a low redox potential which allows radiation-induced hydrated electrons to flow to texaphyrin rather than neutralizing hydroxyl radicals, allowing hydroxyl radicals to cause cellular damage, ii) a relatively stable texaphyrin radical that reacts readily to covalently modify neighboring molecules causing further cellular damage, iii) intrinsic biolocalization, and iv) indifference to the presence or absence of O2. These properties allow texaphyrins to be particularly effective for treating the hypoxic areas of solid neoplasms. Methods of treatment for an individual having a neoplasm or atheroma include the use of a texaphyrin as a radiation sensitizer and as an agent for photodynamic tumor therapy, or the use of a texaphyrin for internal and for external ionizing radiation. Novel texaphyrins are provided.

대표청구항 ▼

A method of magnetic resonance image enhancement in a subject, the method comprising: administering to the subject an effective amount of a paramagnetic texaphyrin complex-oligonucleotide conjugate; and imaging the subject using a magnetic resonance device; wherein the texaphyrin has structure A or

A method of magnetic resonance image enhancement in a subject, the method comprising: administering to the subject an effective amount of a paramagnetic texaphyrin complex-oligonucleotide conjugate; and imaging the subject using a magnetic resonance device; wherein the texaphyrin has structure A or B: [Figure] [Figure] wherein, M is a paramagnetic metal cation; 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, aminoalkyl, oxyaminoalkyl, 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, aminoalkyl, oxyaminoalkyl, carboxyalkyl, carboxyamidealkyl or a couple to a site-directing molecule; where, at least one of R1-R10 is an oligonucleotide or a couple to an oligonucleotide; 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; where R5 and R10 are other than hydrogen, then R6 and R9 are hydrogen, hydroxyl, or halide other than iodide; and N is zero, 1 or 2.