This Perspective is a continuation of our analysis of US FDA-approved small-molecule drugs
(1938–2012) containing nitrogen heterocycles. In this study we report drug structure and …

Cyclic peptides are fascinating molecules abundantly found in nature and exploited as
molecular format for drug development as well as other applications, ranging from research …

Macrocycles are one of nature's preferred choices to generate large but cell-permeable
bioactive molecules. Macrocyclization is increasingly prominent in medicinal chemistry …

Achieving oral bioavailability with Proteolysis Targeting Chimeras (PROTACs) is a key
challenge. Here, we report the in vivo pharmacokinetic properties in mouse, rat, and dog of …

Discovering new bioactive molecules is crucial for drug development. Finding a hit
compound for a new drug target usually requires screening of millions of molecules. Affinity …

Synthetic application of asymmetric catalysis relies on strategic alignment of bond
construction to creation of chirality of a target molecule. Remote desymmetrization offers …

Molecular chameleons possess a flexibility that allows them to dynamically shield or expose
polar functionalities in response to the properties of the environment. Although the concept …

The development of potent, specific, and pharmacologically viable chemical probes and
therapeutics is a central focus of chemical biology and therapeutic development. However, a …

Macrocycles fascinate chemists due to both their structure and their applications. However,
we still lack efficient and sustainable synthetic methods, giving us straightforward access to …

Macrocycles are important drug leads with many advantages including the ability to target
flat and featureless binding sites as well as to act as molecular chameleons and thereby …