Natural products (NPs) are a significant source of inspiration towards the discovery of new
bioactive compounds based on novel molecular scaffolds. However, there are currently only …

Fragment-based drug discovery is an important and increasingly reliable technology for the
delivery of clinical candidates. Notably, however, sp3-rich fragments are a largely untapped …

Catalytic intermolecular olefin hydroamination is an enabling synthetic strategy that offers
direct and atom-economical access to a variety of nitrogen-containing compounds from …

The catalytic union of amides, sulfonamides, anilines, imines, or N-heterocycles with a broad
spectrum of electronically and sterically diverse alkyl bromides has been achieved via a …

Metallaphotoredox cross-coupling is a well-established strategy for generating clinically
privileged aliphatic scaffolds via single-electron reactivity. Correspondingly, expanding …

Through evolution, nature has provided natural products (NPs) as a rich source of diverse
bioactive material. Many drug discovery programs have used nature as an inspiration for the …

Current fragment-based drug design relies on the efficient exploration of chemical space by
using structurally diverse libraries of small fragments. However, structurally dissimilar …

Fragment-based drug discovery (FBDD) is a well-established approach for the discovery of
novel medicines, illustrated by the approval of two FBBD-derived drugs. This methodology is …

Abstract Pseudo‐natural‐product (NP) design combines natural product fragments to
provide unprecedented NP‐inspired compounds not accessible by biosynthesis, but …

In fragment-based drug discovery, hundreds or often thousands of compounds smaller
than~ 300 Da are tested against the protein of interest to identify chemical entities that can …