Diversity-Oriented Synthesis of Conformationally C.. (DOS-peptidomimetics)
Diversity-Oriented Synthesis of Conformationally Constrained Peptidomimetics
Date du début: 6 oct. 2014,
Date de fin: 5 oct. 2016
There is an undoubted need of new small molecule libraries with high levels of scaffold diversity in order to address challenging ‘undruggable’ biological targets which have proven largely intractable to small molecule modulation using traditional compound libraries. The efficient de novo generation of such collections presents a formidable challenge to the synthetic chemist; over the course of the last decade diversity-oriented synthesis has established itself as a powerful tool in this regard. The research outlined in this Marie Curie Fellowship proposal is advancing the impact that synthetic organic chemistry will have on the drug discovery process employing diversity-oriented synthesis. We proposed the preparation of a novel and diverse library of conformationally constrained peptidomimetics containing quaternary stereocenters derived from B/C/P approach with increased biological relevance. In order to provide a visually accessible representation of the abstract concepts of chemical space and the molecular diversity of our new chemical libraries a computational assessment will be developed. As a final step, the small-molecules obtained will be screened to identify new molecular targets against cancer and infectious diseases. This is a multidisciplinary project that involves a highly valuable education for the candidate in new scientific aspects related to her research field.
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