Abstract The Stimulator of Interferon Genes (STING) plays an important role in innate immunity by inducing type I interferons response to sensing viral or bacterial cytosolic DNA. Cyclic dinucleotides (CDNs) are known activate STING. Here, we describe the synthesis and biological evaluation two new 3’,3’‐CDN, which internucleotide linkages were replaced, respectively, a 1,2,3‐triazole moiety (a...

A new strategy is described to generate bicyclic peptides that incorporate non-peptidic backbone elements starting from recombinant polypeptide precursors. These compounds are produced via a one-pot, two-step sequence, in which peptide macrocyclization by means of a bifunctional oxyamine/1,3-amino-thiol synthetic precursor is followed by intramolecular disulfide formation between the synthetic ...

N,N'-bis(bromobenzyl) and N,N'-bis(halopyridinyl) derivatives of diaza-12-crown-4, diaza-15-crown-5 and diaza-18-crown-6 ethers were synthesized in high yields. The Pd-catalyzed macrocyclization reactions of these compounds were carried out using a variety of polyamines and oxadiamines were carried out to give novel macrobicyclic and macrotricyclic compounds of the cryptand type. The dependence...

Metallosupramolecular squares have been successfully evolved over the past years as versatile substitutes of the conventional organic macrocycles owing to the development of reliable synthetic protocols and abundant structural variability (metals and ligands). In this review we have presented the fundamental aspects of metallosupramolecular squares such as the strategies for their construction ...

Arylomycins are a promising class of "latent" antibacterial natural products currently in preclinical development. Access to analogues within this family has previously required a lengthy route involving multiple functional group manipulations that is costly and time-intensive on scale. This study presents a simplified route predicated on simple C-H functionalization logic that is enabled by a ...

Macrocycles are interesting molecules because their topological features and constrained properties significantly affect their chemical, physical, biological, and self-assembling properties. In this report, we synthesized unique macrocyclic peptides composed of both an α-helix and a polyproline segment and analyzed their conformational properties. We found that the molecular stiffness of the ro...

Embedding seven-membered rings into polycyclic aromatic molecules is attractive as they can exert an influence on molecular conformation that ultimately changes the solubility and π-electronics. The considerations in designing synthesizing a highly strained azatriseptane framework are discussed herein. We employ twofold macrocyclization strategy to form [7,7,7]-system through scoping various st...

(-)-Lyngbyaloside B is a 14-membered macrolide glycoside isolated from the marine cyanobacterium Lyngbya sp. as a cytotoxic substance by Moore and co-workers. The first total synthesis of (-)-lyngbyaloside B and the reassignment of its stereostructure is described. The synthesis features an Abiko-Masamune aldol reaction, a vinylogous Mukaiyama aldol reaction, and a macrocyclization involving an...