The overarching objective of this project is the improvement of treatment outcomes for cancer patients who require chemotherapy. An important class of chemotherapeutic agents is that of platinum-containing antineoplastic drugs. The treatment is typically associated with numerous side effects and the risk of malignancies which develop drug resistance.<br/>Here the synthesis of new ligands for platinum complexes derived from indoles is described. The complexes are designed to facilitate DNA-bending upon base crosslinking. The DNA-platinum adducts will be characterized to gain insight into the mechanisms of DNA-related cytotoxicity of these platinum compounds and to conduct cell-imaging studies.<br/>The new ligands are obtained from nitroanilines through Fischer indole synthesis followed by Mannich reactions to introduce side chains. These are designed to modify the lipophilicity of ligands, contribute some steric hindrance and can be functionalized to attach reporter groups to determine the position of the adduct on the DNA as well as the location in the cell.<br/>Synthetic methodologies, procedures for the separation of enantiomeric products and analyses of platinum compounds are presented.

Synthesis of novel ligands for platinum drugs

254th National Meeting (2017)

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