UCLA researchers in the Department of Chemistry and Biochemistry have developed a small molecule library consisting of a large variety stereochemical variants.
Small molecule libraries are used for high throughput screening for any biological activity. These are used for drug discovery and to investigate mechanisms of activity. However, current libraries are composed of common molecules and their variants and do not include the vast majority of chemical conformations. There is an unmet need for libraries than sample a large number of backbone conformations and stereochemical diversity.
UCLA researchers have developed a method to synthesize a chemical library composed of unique molecules. Their ‘diversity-oriented synthesis’ technique was used to generate a 91-molecule library. The library consists of heterocyclic compounds composed of 16 distinct scaffolds and samples a large variety of structural and stereochemical conformations. They have used it to screen for inhibitors of invasion properties of breast cancer cells and have discovered 3 lead compounds. Additionally, the library has been screened for inhibitors of T cell exocytosis and for IFN-γ-like compounds.
Chemical library designed and synthesized
Utilized to screen for:
|United States Of America||Issued Patent||8,624,032||01/07/2014||2012-293|
Chemical biology, diversity-oriented synthesis, heterocycles, synthesis design, high throughput screening, small molecule library