α-Amanitin is an extremely toxic bicyclic octapeptide isolated from the death-cap mushroom,
Amanita phalloides. As a potent inhibitor of RNA polymerase II, α-amanitin is toxic to …

For 70 years, α-amanitin, the most cytotoxic peptide in its class, has been without a synthetic
rival; through synthesis, we address the structure–activity relationships to inform the design …

Appreciating the need to access synthetic analogs of amanitin, here we report the synthesis
of 5′-hydroxy-6′-deoxy-amanitin, a novel, rationally-designed bioactive analog and …

Targeted cancer therapy represents a paradigm-shifting approach that aims to deliver a
toxic payload selectively to target-expressing cells thereby sparing normal tissues the off-target …

Indole dearomatization of tryptophan represents a key approach in the synthesis of indole
containing alkaloids. Although the reactivity of C-3a-bromo-, 3a-iodo-, and 3a-…

Antibody–drug conjugates (ADCs) constitute an emerging class of anticancer agents that
deliver potent payloads selectively to tumors while avoiding systemic toxicity associated with …

Here we report a scalable synthesis of the key amino acid residue, (2S,3R,4R)-4,5-dihydroxyisoleucine
(DHIle) in α-amanitin, that in turn enables the scalable synthesis of an equipotent …

Alpha‐amanitin is an exceedingly toxic, naturally occurring, bicyclic octapeptide that inhibits
RNA polymerase and results in cellular and organismal death. Here we report the …

After the identification of the high-affinity glutamate-ureido scaffold, the design of several
potent 18 F- and 68 Ga-labeled tracers has allowed spectacular progress in imaging recurrent …

Sulfilimines, as potential aza‐isosteres of sulfoxides, are valued as building blocks, auxiliaries,
ligands, bioconjugation handles, and as precursors to versatile S(VI) scaffolds including …