Jump to main content
Jump to site search
Access to RSC content Close the message box

Continue to access RSC content when you are not at your institution. Follow our step-by-step guide.


Issue 35, 2011
Previous Article Next Article

The rise, fall and reinvention of combinatorial chemistry

Author affiliations

Abstract

Combinatorial chemistry provides a powerful tool for the rapid creation of large numbers of synthetic compounds. Ideally, these libraries should be a rich source of bioactive molecules, but there is the general feeling that the initial promise of combinatorial chemistry has not yet been realized. In particular, enthusiasm for conducting unbiased (non-structure-guided) screens of large libraries for protein or RNA ligands has waned. A central challenge in this area is to devise methods for the synthesis of chemically diverse, high-quality libraries of molecules with many of the desirable features of natural products. These include diverse functionality, a significant representation of chiral sp3 centers that provide conformational bias to the molecule, significant skeletal diversity, and good pharmacokinetic properties. However, these libraries must be easy to make from cheap, readily available building blocks, ideally those that would support convenient hit optimization/structure reactivity relationship studies. Meeting these challenges will not be easy. Here I review some recent advances in this area and provide some thoughts on likely important developments in the next few years.

Graphical abstract: The rise, fall and reinvention of combinatorial chemistry

Back to tab navigation

Article information


Submitted
12 Apr 2011
Accepted
24 May 2011
First published
24 Jun 2011

Chem. Commun., 2011,47, 9757-9763
Article type
Highlight

The rise, fall and reinvention of combinatorial chemistry

T. Kodadek, Chem. Commun., 2011, 47, 9757
DOI: 10.1039/C1CC12102B

Social activity

Search articles by author

Spotlight

Advertisements