Periodic Reporting for period 1 - SYNFOS (Synthetic toolkit for fragment oriented synthesis)
Période du rapport: 2018-03-01 au 2020-02-29
Direct fragment growth will not only contribute to improve productivity of early stages drug development by reducing the synthetic burden, but also will allow to navigate through unexplored chemical space. In particular, the exploitation of molecules with increased tridimensionality has been linked to the discovery of drug candidates with higher probabilities of reaching the market. Hence, the research proposed for the current action will contribute with know-how to the global efforts of targeting new diseases by providing new better drugs while increasing pipeline productivity.
The overall objective of the action is the development of a synthetic toolbox that facilitates the introduction of a range of medicinally-relevant functionalities into fragment molecules through their direct activation. The toolbox usefulness will be demonstrated by the discovery of new bioactive molecules able to interact with protein function.
Two of the three new reactions will be submitted for publishing featuring only synthetic studies, whilst the third method is expected to be published in the following year in combination with the fragment hit elaboration for Aurora A kinase. At the moment of closure of the fellowship, to protect the know-how no public presentation on seminars/congress or other forms of dissemination had been delivered. Nevertheless, the project achieved important dissemination actions through informal closed meetings with fragments end users, companies that focus on fragment-based drug discovery to drive drug development pipelines, where the findings were reported through oral presentation.