Synthesis, Antitumor and Antibacterial Studies of New Shortened Analogues of (KLAKLAK)₂-NH₂ and Their Conjugates Containing Unnatural Amino Acids.

ABSTRACT: (1) Background: (KLAKLAK)₂ is a representative of the antimicrobial peptide group which also shows good anticancer properties. (2) Methods: Herein, we report synthesis using SPPS and characterization by HPLC/MS of a series of shortened analogues of (KLAKLAK)₂. They contain single sequence KLAKLAK as C-terminal amides. In addition, substitution of some natural amino acids with unnatural β-Ala and nor-Leu is realized. In addition, these structures are conjugated with second pharmacophore with well proven anticancer properties 1,8-naphthalimide or caffeic acid. Cytotoxicity, antiproliferative effect and antimicrobial activity of newly synthesized structures were studied. (3) Results: The obtained experimental results reveal significant selective index for substances with

SUBMITTER: Jaber S 

PROVIDER: S-EPMC7915940 | biostudies-literature | 2021 Feb

REPOSITORIES: biostudies-literature