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Since its discovery in 1928 by Diels and Alder, 1 the Diels–Alder reaction has become one
of the cornerstone reactions in organic chemistry for the construction of six-membered rings …

Criteria for predicting the druglike properties of “beyond Rule of 5” Proteolysis Targeting
Chimeras (PROTAC) degraders are underdeveloped. PROTAC components are often …

We report an atomistic physical model for the passive membrane permeability of cyclic
peptides. The computational modeling was performed in advance of the experiments and …

A collection of structurally complex and chemically diverse small molecules is a useful tool to
explore cell circuitry. In this article, we report the split-pool synthesis of more than 3000 …

Natural products are central to biology and medicine, serving as pharmaceutical leads,
drugs, 4 and powerful reagents for studying cell biology. 5 To date, libraries based upon …

Small-molecule synthesis coupled with cellular profiling using multidimensional screening
can be used to assess the impact of varying stereochemical and appendage contexts on …

The efficient synthesis of small molecules having many molecular skeletons is an unsolved
problem in diversity-oriented synthesis (DOS). We describe the development and …

Diversity-oriented synthesis of structurally complex and diverse small molecules can be
used as the first step in a process to explore cellular and organismal pathways. The success …

Natural products that act as highly specific, small-molecule protein-binding agents and as
modulators of protein-protein interactions are highly complex and exhibit functional groups …