Since Hedin's characterization of trypsin and antitrypsin in 1906,(1) arguably the first
account of a regulatory protein–protein interaction (PPI), contemporary understanding of …

Conspectus Cycloaddition reactions are among the most powerful methods for the synthesis
of complex compounds. In particular, the development and application of the 1, 3-dipolar …

In the search for new therapeutic agents for currently incurable diseases, attention has
turned to traditionally “undruggable” targets, and collections of drug-like small molecules …

For scientists to gain a better understanding of nature, biological research is greatly aided by
small-molecule modulators that perturb protein activity without fundamentally altering the …

Covering: up to 2013 Natural products and their derivatives are used as treatments for
numerous diseases. Many of these compounds are structurally complex, possessing a high …

High-throughput screening has become a mainstay of small-molecule probe and early drug
discovery. The question of how to build and evolve efficient screening collections …

Many compound screening collections are populated by members that possess a low
degree of structural complexity. In an effort to generate compounds that are both complex …

The current state of affairs in the drug discovery and development process is briefly
summarized and then ways to take advantage of the ever‐increasing fundamental …

Highlights•Twenty-four libraries generated using natural products as guiding structures were
analyzed.•The variation of two main lead-like descriptors (MW, logP) within the libraries was …

Screening of small-molecule libraries is an important aspect of probe and drug discovery
science. Numerous authors have suggested that bioactive natural products are attractive …