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Project

Structural optimization of MEL-6 and development towards a prostate cancer therapeutic

Resistance to the current androgen receptor antagonist is a growing problem when treating prostate cancer patients. Therefore, new inhibitors of the androgen receptor are required to have an alternative mechanism of action or a different structure. MEL-6 was identified as a compound with excellent properties on in vitro models of prostate cancer resistance and moreover has a completely different structure compared to the current antiandrogens. Unfortunately, the half life of MEL-6 was estimated to be only 4 minutes which is insufficient to garantee activity in mouse models. In this project we aim to optimize the structure of MEL-6 via 4 different synthesis strategies in order to improve its metabolic stability. MEL-6 derivatives with activity on in vivo mouse models of prostate cancer will be protected with a patent. In collaboration with the farmaceutical industry we would like to perform clinical studies in the department of Urology of the UZ Leuven.
Date:1 Oct 2015 →  30 Sep 2017
Keywords:prostate cancer
Disciplines:Morphological sciences, Oncology