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Theranostics Targeting Metastatic Breast Cancer

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Technical Report,30 Sep 2015,29 Sep 2016

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Methodist Hospital Houston United States

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The emphasis of this first year of the award, as planned, has been on synthetic chemistry to obtain materials to test in histology, PET positron emission tomography and PDT photodynamic therapy studies. We have been successful in preparing samples for the testing studies that begin in year 2. However, as anticipated, the synthetic chemistry work was not without problems and must continue and adapt to overcome challenges that now become evident. For instance, one of the molecules first prioritized, compound 1, was prepared, but only after a great deal of effort in retrospect it is now clear that this compound has stability issues that make it hard to make, and inappropriate for further studies. Another target compound 2 was then prepared, much more efficiently than the first because it does not have stability issues, and because of the experience we gained from making the first target. This compound has poor solubility characteristics despite the fact that it contains two sulfonic acid groups and may required delivery in micelles this is something that could not have been predicted until the compound was made. Both structures 1 and 2 are based on the aza-BODIPY dye fragment as a back-up we have also initiated work on a compound based on a different-dye type, eg compound 3. The original proposal outlined plans to add cytotoxic entities other than PDT agents for this we entered into a collaboration with a biotechnology company who have provided us a small sample of the previous, highly cytotoxic, compound maytensin A. We have also prepared an agent intended solely for PET, i.e. compound 4 this takes advantage of very recent advances in the field that enable more efficient capture of 18F- than was possible before, via so-called Perrin capture agents.

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  • Medicine and Medical Research

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