主权项 |
1. A Dual Nuclear/NIR Agent having a structure according to one of the following formulas: wherein R1 and R2 are each independently selected from the group consisting of radioisotopes I-125, I-123, I-131, I-124, F-18, hydrogen, sulfonato, an electron withdrawing group (EWG), an electron donating group (EDG), and are each independently attached at any of the aromatic ring positions; R3 and R4 are independently selected from the group consisting of hydrogen, alkyl, aryl, aralkyl, alkylsulfonato, alkylcarboxylic, alkylamino, ω-alkylaminium, ω-alkynyl, PEGyl, PEGylcarboxylate, ω-PEGylaminium, ω-acyl-NH—CR, ω-acyl-lysine-CR, ω-acyl-triazole-CR, ω-PEGylcarboxyl-NH—CR, ω-PEGylcarboxyl-lysine-CR, and ω-PEGylcarboxyl-triazole-CR; X is selected from the group consisting of a hydrogen, halogen, I-125, I-123, I-131, I-124, F-18, CN, Me, OH, 4-O-Ph-CH2CH2COOH, 4-O-Ph-NH—CR, NH—CR, 4-S-Ph-NH—CR, ω-iminoacyl-NH—CR, ω-aminoacyl-lysine-CR, ω-iminoacyl-triazole-CR, 4-O-Ph-CH2CH2COOCT, 4-O-Ph-O-CT, 4-S-Ph-O-CT, and ω-iminoacyl-O-CT, wherein CR is selected from the group consisting of a metal chelating agent, a radioactive or nonradioactive metal complex, a radioiodine or iodine labeled Bolten-Hunter reagent, and a radioiodine or iodine labeled tyrosine moiety, wherein the metal is selected from the group consisting of Cu-64, In-111, Tc-99m, Ga-68, Y-90, Lu-177, Re-188, At-211, Bi-213, Ac-225 and their nonradioactive counterparts, wherein CT is selected from the group consisting of radiolabeled or non-radiolabeled cytotoxic drugs, antibodies, toxins, aptamers, siRNA, antisense constructs and microRNAs; and counteranion A is selected from the group consisting of iodide, bromide, arylsulfonato, alkylsulfonato, tetrafluoroborate, chloride, and a pharmaceutically acceptable anion. |