Abstract: The present invention relates to non-membrane disruptive and p53 activating stapled peptides, as well as methods of treatment of cancer involving the use of these peptides. In one embodiment, the peptide comprises or consist of the amino acid sequence of TSFXaa1EY-WXaa3LLXaa2, where Xaa1 is (R)-2-(7?-octenyl)alanine or derivative thereof, or is (R)-2-(4?-pentenyl)alanine or derivative thereof; and Xaa2 and Xaa3 are independently any type of amino acid or modified amino acid. In another embodiment, the peptide comprising or consisting of the amino acid sequence of TSFXaa1EYW Xaa3LLXaa2ENXaa5, wherein Xaa1 and Xaa3 are any type of amino acid or modified amino acid; Xaa2 is S, or P, or (S)-2-(4?-pentenyl)alanine or a derivative of (S)-2-(4?-pentenyl)alanine; and wherein Xaa5 is F or Y.

Abstract: This invention relates to a process for producing a compound of Formula I, comprising: 1) performing a stereoselective metathesis reaction on a compound of Formula II so as to form an intramolecular alkenyl chain, and 2) cleaving S from P2 so as to produce a compound of Formula I. A product containing an (Z)- or (E)-olefin isomer stabilised in an a-helical conformation is obtained by the said process.

Abstract: The present invention relates to non-membrane disruptive and p53 activating stapled peptides, as well as methods of treatment of cancer involving the use of these peptides. In one embodiment, the peptide comprises or consist of the amino acid sequence of TSFXaa1EYWXaa3LLXaa2, where Xaa1 is (R)-2-(7?-octenyl)alanine or derivative thereof, or is (R)-2-(4?-pentenyl)alanine or derivative thereof; and Xaa2 and Xaa3 are independently any type of amino acid or modified amino acid. In another embodiment, the peptide comprising or consisting of the amino acid sequence of TSFXaa1EYW Xaa3LLXaa2ENXaa5, wherein Xaa1 and Xaa3 are any type of amino acid or modified amino acid; Xaa2 is S, or P, or (S)-2-(4?-pentenyl)alanine or a derivative of (S)-2-(4?-pentenyl)alanine; and wherein Xaa5 is F or Y.