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A Diversity-Oriented Synthesis for the Generation of Diverse Natural-like Compounds

Carlsbergfondets internationaliseringsstipendier

What

Traditionally, screening processes are based on huge collections of structurally simple and similar compounds, although it has recently become the generally consensus, that structurally diversity, rather than the size of the compounds collection is important. In this project, we want to develop a protocol that allows for the generation of a diverse compound collection constructed from a simple accessible starting material. This compound collection will provide us with highly diverse scaffolds with nature-like fragments. Hereby, we will get access to compounds that are promising drug candidates. We will test the compounds for their activity for the treatment of resistant infections and cancer.

Why

Antimicrobial drugs have been overused extensively in the last decade, which have resulted in high drug resistance against common infections. Moreover, poor toxicity profiles of many anticancer drugs is problematic which leads to detrimental adverse effects. Therefore, there is a need for developing selective anticancer drugs and antimicrobial drugs. In this project, we will provide a compound selection consisting of structural diverse scaffolds. We will test against relevant biological interesting targets to provide better treatment for cancer and infections.

How

This proposal will be carried out with Prof. David R. Spring at the University of Cambridge, UK. The Spring has high experience with diversity-oriented synthesis programs, which will provide me with the needed expertise and knowledge that will guaranty a successful outcome of the project.

SSR

We will develop a method for the synthesis of structural diverse, nature-like compounds. These are promising candidates as biological active compounds. Therefore, this may lead to the identification of new drug candidates, which will increase the life quality of affected people. Furthermore, this will also have a high economical value for the society, as the diseased persons will need shorter hospitalisations.