title: Synthesis of anticancer heptapeptides containing a unique lipophilic β(2,2) -amino acid building block.
abstract: We report a series of synthetic anticancer heptapeptides (H-KKWβ(2,2) WKK-NH(2)) containing eight different central lipophilic β(2,2) -amino acid building blocks, which have demonstrated high efficiency when used as scaffolds in small cationic antimicrobial peptides and peptidomimetics. The most potent peptides in the present study had IC(50) values of 9-23 µm against human Burkitt's lymphoma and murine B-cell lymphoma and were all nonhaemolytic (EC(50)  > 200 µm). The most promising peptide 10e also demonstrated low toxicity against human embryonic lung fibroblast cells and peripheral blood mononuclear cells and exceptional proteolytic stability.
authors.affiliation: Department of Pharmacy, Faculty of Health Sciences, University of Tromsø, NO-9037, Tromsø, Norway.
authors.forename: Veronika
authors.initials: V
authors.lastname: Tørfoss
authors.forename: Dominik
authors.initials: D
authors.lastname: Ausbacher
authors.forename: Cristiane de A
authors.initials: Cde A
authors.lastname: Cavalcanti-Jacobsen
authors.forename: Terkel
authors.initials: T
authors.lastname: Hansen
authors.forename: Bjørn-Olav
authors.initials: BO
authors.lastname: Brandsdal
authors.forename: Martina
authors.initials: M
authors.lastname: Havelkova
authors.forename: Morten B
authors.initials: MB
authors.lastname: Strøm
mesh_terms: D000596:Amino Acids / Q000737:chemistry*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D002051:Burkitt Lymphoma; D045744:Cell Line, Tumor; D006801:Humans; D020128:Inhibitory Concentration 50; D007963:Leukocytes, Mononuclear; D016393:Lymphoma, B-Cell; D051379:Mice; D009842:Oligopeptides / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D000596:Amino Acids; D000970:Antineoplastic Agents; D009842:Oligopeptides