Thiopeptides, or thiazolyl peptides, are a relatively new family of antibiotics that already counts with more than one hundred different entities. Although they are mainly isolated from soil bacteria, during the last decade, new members have been isolated from marine samples. Far from being limited to their innate antibacterial activity, thiopeptides have been found to possess a wide range of biological properties, including anticancer, antiplasmodial, immunosuppressive, etc. In spite of their ribosomal origin, these highly posttranslationally processed peptides have posed a fascinating synthetic challenge, prompting the development of various methodologies and strategies. Regardless of their limited solubility, intensive investigations are bringing thiopeptide derivatives closer to the clinic, where they are likely to show their veritable therapeutic potential.

The latest developments towards the synthesis of lamellarins, their structure–activity relationship and advances in the mechanism of action are described.

The pyrrolo[2,3-c]carbazole 1, the common core of the marine alkaloids known as the dictyodendrins, has been synthesised. The sequence is based on a Suzuki cross-coupling reaction between the pyrrole fragment 2 and the indole fragment 3, followed by tandem photochemical 6π-electrocyclisation/aromatisation.