‘Modular Synthetic Platform for Elaborating Fragments to 3-D Lead Compounds for Fragment Based Drug Discovery’

Hosts: Jeff Wong / Olga Semenova 

Venue: MSI Small Lecture Theatre, SLS 

Abstract:   

Over the past 20 years, fragment-based drug discovery (FBDD) has become a well-established method for hit and lead generation. To date, six approved drugs have originated from FBDD campaigns. These drugs comprise 2-D heteroaromatics which likely reflects that there is a high proportion of 2-D fragments in typical fragment libraries. There is increasing interest in exploring novel 3-D pharmaceutical space. However, the elaboration of a 2-D fragment hit to a 3-D lead compound can be challenging: researchers at Astex have noted that “ideally it should be possible to synthetically elaborate fragments in 3 dimensions from many different growth points/vectors using methodology that is worked out prior to fragment screening“. To address this, we are developing a modular synthetic platform for the elaboration of 2-D fragment hits (e.g. FragLites) into 3-D lead-like compounds. This will be achieved using synthetically-enabled bifunctional 3-D building blocks with distinct 3-D elaboration vectors. The use of this synthetic platform in the discovery of a novel and selective JAK3 inhibitor will be presented.  

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