Activity Directed Synthesis for the discovery of small bioactive molecules


Conventional small-molecule discovery approaches are both time consuming and resource inefficient. These approaches involve the synthesis, purification and screening of many individual molecules, using a limited palette of reliable and well-established chemical transformations. Hence, all molecules are treated with the same significance irrespective of their ultimate biological activity. We present a novel evolutionary approach which is highly efficient and focuses only on active compounds: sequential rounds of promiscuous carbenoid reactions, screening of unpurified reaction mixtures and selection of the most productive conditions, lead to the rapid discovery of small-molecule modulators of a known biological target, based on a novel scaffold.3 The approach allows for the parallel optimisation of both the structure of the bioactive molecule and a route for its synthesis. Sub-micromolar, chemically unprecedented and biologically novel modulators of a known biological target have been discovered using this newly developed methodology.

Hosted By

The European Laboratory Research & Innovation Group Our Vision : To provide outstanding, leading edge knowledge to the life sciences community on an open access basis
Event Logo Follow us on Twitter

Get the App

Get this event information on your mobile by
going to the appstore or google play and search for 'elrig'
Eventflo Home
copyright ELRIG,, Labhoo Ltd 2003-2021