Diversity-oriented synthesis as a tool for the discovery of novel biologically active small molecules.
Biologically active molecules can be identified through the screening of small-molecule libraries. Deficiencies in current compound collections are evidenced by the continuing decline in drug-discovery successes. Typically, such collections are comprised of large numbers of structurally similar compounds. A general consensus has emerged that library size is not everything; library diversity, in terms of molecular structure and thus function, is crucial. Diversity-oriented synthesis (DOS) aims to generate such structural diversity in an efficient manner. Recent years have witnessed significant achievements in the field, which help to validate the usefulness of DOS as a tool for the discovery of novel, biologically interesting small molecules.
Galloway
Warren R J D
WR
The University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, England, UK.
Isidro-Llobet
Albert
A
Spring
David R
DR
D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D055808:Drug Discovery / Q000379:methods*; D015394:Molecular Structure; D054852:Small Molecule Libraries
D054852:Small Molecule Libraries