Design and synthesis of 14 and 15-membered macrocyclic scaffolds exhibiting inhibitory activities of hypoxia-inducible factor 1α

Brønsted Acid-Catalyzed Cascade Ring-Opening/Cyclization of 3-Ethoxy Cyclobutanones to Access 2,8-Dioxabicyclo[3.3.1]nonane Derivatives

“…This type of heteroatom-containing complex 15-membered macrocycle could be found in biologically important molecules and could be utilized as metal ion recognition and complexing agents. It could also show antitumor and inhibitory activities . Here, it is worth noting that only the intramolecular cyclization happened in which 3afa was obtained with a 3:2 ratio of trans and cis isomers, and no intermolecular cyclization product was detected.…”

Comprehensive exploration of chemical space using trisubstituted carboranes

“…We developed tricyclic three-dimensional scaffolds that are rich in sp 3 -hybridized carbon centres to access unexplored chemical spaces, and we used these scaffolds to design peptidomimetic molecules 33 – 35 . The α-helix is one of the important elements of a protein’s secondary structure that affords the construction of three-dimensional tertiary structures of proteins.…”

Peptide-encoding gene transfer to modulate intracellular protein-protein interactions

“…Moreover, the process of optimization from a lead compound is time consuming. 42 Recent advances in substitution with unnatural amino acids 39 ; the introduction of sidechain linkers, 9 which were reported to be useful not only for stability but also for affinity enhancement 43 ; and the development of macrocyclization 44 enable the further potentiation of peptide drugs. We previously found an association between DDX6 and 4ET, which plays a central role in RNA decay in RNA metabolism.…”