Comparative Positron-Emission Tomography (PET) Imaging and Phototherapeutic Potential of 124I- Labeled Methyl- 3-(1'-iodobenzyloxyethyl)pyropheophorbide-a vs the Corresponding Glucose and Galactose Conjugates.

[摘要]：In our present study, 3-(1'-m-iodobenzyloxyethyl)pyropheophorbide-a Me ester 1, 3-(1'-m-iodobenzyloxyethyl)-172-{(2-deoxy)glucose}pyropheophorbide- a 2, and 3-(1'-m-iodobenzyloxyethyl)-172-{(1-deoxy)galactose}pyropheophorbid e-a 3 were synthesized and converted into the corresponding 124I-labeled analogs by reacting the intermediate trimethyltin analogs with Na124I. Photosensitizers 1-3 were evaluated for the PDT efficacy in C3H mice bearing RIF tumors at variable doses and showed a significant long-term tumor cure. Among the compds. investigated, the non-carbohydrate analog 1 was most effective. These results were in contrast to the in vitro data, where compared to the parent analog the corresponding galactose and glucose derivs. showed enhanced cell kill. Among the corresponding 124I-labeled analogs, excellent tumor images were obtained from compd. 1 in both tumor models (RIF and Colon-26) and the best tumor contrast was obsd. at 72 h after injection. Conjugating a glucose moiety to photosensitizer 1 initially diminished its tumor uptake, whereas with time the corresponding galactose analog showed improved tumor contrast.

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