Biocompatible Technologies for the Radiolabeling and Synthesis of Chemotherapeutics: The state-of-the-art methods for the isotopic labelling and synthesis of new cancer therapeutics has been limited to precious metal catalysts which exhibit high toxicity. Sustainable methods to generate promising therapeutic candidates are necessary to advance the field of cancer therapy and diagnostics. This work is focused on biocompatible methods for radiolabeling of drug candidates with several isotopes, specifically deuterium and tritium (Aim 1) and fluorine-18 (Aim 2) for oncology studies and diagnostic imaging. Synthetic methods using these biocompatible precursors will be explored to generate innovat...

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Biocompatible Technologies for the Radiolabeling and Synthesis of Chemotherapeutics: The state-of-the-art methods for the isotopic labelling and synthesis of new cancer therapeutics has been limited to precious metal catalysts which exhibit high toxicity. Sustainable methods to generate promising therapeutic candidates are necessary to advance the field of cancer therapy and diagnostics. This work is focused on biocompatible methods for radiolabeling of drug candidates with several isotopes, specifically deuterium and tritium (Aim 1) and fluorine-18 (Aim 2) for oncology studies and diagnostic imaging. Synthetic methods using these biocompatible precursors will be explored to generate innovative small-molecule fragments for exploration as potential chemotherapeutics (Aim 3). Aim 1: Deuteration and Trituration of Anticancer Drugs for Drug Discovery and Development Goals and Objectives. Our work intends to develop new HIE catalysts with biocompatible earth abundant metals, like magnesium and calcium, to facilitate the deuteration of common functional motifs in pharmaceuticals such as arenes and nitrogen-based heterocycles. Aim 2: Designing Site-Selective Fluorination Radiolabeling Protocols for Diagnostic Imaging Goals and Objectives. Technologies for the late-stage 19F/18F conversion of chemotherapeutics represents a growing area of need to access clinically relevant PET agents. We will meet this need by developing new synthetic methods to translate fluorinated anticancer drugs into radiotracers. Aim 3: Creating Structurally Diverse Molecular Complexity for Fragment-based Library Discovery Goals and Objectives. The use of fragment-based methods has arisen as an attractive and indispensable strategy for approaching early-stage drug development and design, however available fragment libraries are limited. We are developing synergistic strategies that access underexplored heterocycles for creating large chemical libraries that will lead to new anticancer therapies.

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