Sidechain structure-activity relationships of cyclobutane-based small molecule αvβ3 antagonists.

The integrin family of cell surface extracellular matrix binding proteins are key to several physiological processes involved in tissue development, as well as cancer proliferation and dissemination. They are therefore attractive targets for drug discovery with cancer and non-cancer applications. We have developed a new integrin antagonist chemotype incorporating a functionalised cyclobutane ring as the central scaffold in an arginine-glycine-aspartic acid mimetic structure.

Encapsulation of echinomycin in cyclodextrin inclusion complexes into liposomes: anti-proliferative and anti-invasive activity in glioblastoma.

Echinomycin, a DNA bis-intercalator peptide, belongs to the family of quinoxaline antibiotics. Echinomycin exhibits potent antitumor and antimicrobial activity. However, it is highly water insoluble and suffers from low bioavailability and unwanted side effects.