• Aldol condensations on a 3-alkylidene-2,5-diketopiperazine - synthesis of two marine natural products 

      Fairhurst, Magnus John E.; Muhammad, Zeeshan; Haug, Bengt Erik; Bayer, Annette (Peer reviewed; Journal article, 2018)
      The synthesis of two marine natural products containing a 3-alkylidene-6-arylidene-2,5-diketopiperazine scaffold by employing two consecutive aldol condensations starting with 1,4-diacetyl-2,5-diketopiperazine is reported. ...
    • Design, synthesis, and biological evaluation of scaffold-based tripeptidomimetic antagonists for CXC chemokine receptor 4 (CXCR4) 

      Zachariassen, Zack Georg; Thiele, Stefanie; Berg, Erik; Rasmussen, Pernille; Fossen, Torgils; Rosenkilde, Mette M.; Våbenø, Jon; Haug, Bengt Erik (Journal article, 2014)
      Structure–activity relationship studies of the cyclopentapeptide CXCR4 antagonists (cyclo(-l-/d-Arg1-Arg2-2-Nal3-Gly4-d-Tyr5-)) suggest that the l-/d-Arg1-Arg2-2-Nal3 tripeptide sequence contained within these cyclopentapeptides ...
    • Influence of chain length on the activity of tripeptidomimetic antagonists for CXC chemokine receptor 4 (CXCR4) 

      Baumann, Markus; Hussain, Mohammad Musarraf; Henne, Nina; Garrote, Daniel Moya; Karlshøj, Stefanie; Fossen, Torgils; Rosenkilde, Mette M.; Våbenø, Jon; Haug, Bengt Erik (Peer reviewed; Journal article, 2017-01)
      Here we report a series of close analogues of our recently published scaffold-based tripeptidomimetic CXCR4 antagonists, containing positively charged guanidino groups in R1 and R2, and an aromatic group in R3. While ...
    • Kinase chemodiversity from the Arctic: the breitfussins 

      Østnes Hansen, Kine; Andersen, Jeanette hammer; Bayer, Annette; Pandey, Sunil Kumar; Lorentzen, Marianne; Jørgensen, Kåre Bredeli; Sydnes, Magne Olav; Guttormsen, Yngve; Baumann, Matthias; Koch, Uwe; Klebl, Bert; Eickhoff, Jan; Haug, Bengt Erik; Isaksson, Johan; Hansen, Espen (Peer reviewed; Journal article, 2019)
      In this work, we demonstrate that the indole-oxazole-pyrrole framework of the breitfussin family of natural products is a promising scaffold for kinase inhibition. Six new halogenated natural products, breitfussin C–H (3 ...
    • LTX-315: a first-in-class oncolytic peptide that reprograms the tumor microenvironment 

      Sveinbjørnsson, Baldur; Camilio, Ketil Andre; Haug, Bengt Erik; Rekdal, Øystein (Peer reviewed; Journal article, 2017)
      The oncolytic peptide LTX-315, which has been de novo designed based on structure–activity relationship studies of host defense peptides, has the ability to kill human cancer cells and induce specific anticancer immune ...
    • Oncolytic peptide LTX-315 induces an immune-mediated abscopal effect in a rat sarcoma model 

      Nestvold, Janne M.; Wang, Mengyu; Camilio, Ketil Andre; Zinöcker, Severin; Tjelle, Torunn Elisabeth; Lindberg, Alf; Haug, Bengt Erik; Kvalheim, Gunnar; Sveinbjørnsson, Baldur; Rekdal, Øystein (Peer reviewed; Journal article, 2017)
      LTX 315 is an oncolytic peptide with potent immunological properties. In the present study, we demonstrate that intratumoral treatment with LTX-315 resulted in a complete regression and systemic immune response in a rat ...
    • Repurposing 18F-FMISO as a PET tracer for translational imaging of nitroreductase-based gene directed enzyme prodrug therapy 

      Ruiz de Garibay, Gorka; García de Jalón, Elvira; Stigen, Endre; Lund, Kjetil B.; Popa, Mihaela-Lucia; Davidson, Ben; Mayoral Safont, Mireia; Rygh, Cecilie Brekke; Espedal, Heidi; Barrett, Torill; Haug, Bengt Erik; Cormack, Emmet Mc (Journal article; Peer reviewed, 2021)
      Nitroreductases (NTR) are a family of bacterial enzymes used in gene directed enzyme prodrug therapy (GDEPT) that selectively activate prodrugs containing aromatic nitro groups to exert cytotoxic effects following gene ...
    • Synthesis of a novel tripeptidomimetic scaffold and biological evaluation for CXC chemokine receptor 4 (CXCR4) antagonism 

      Baumann, Markus; Nome, Lina Marie; Zachariassen, Zack Georg; Karlshøj, Stepfanie; Fossen, Torgils; Rosenkilde, Mette M.; Våbenø, Jon; Haug, Bengt Erik (Peer reviewed; Journal article, 2017-07)
      We here report the preparation of a new 2,6,8-trisubstituted bicyclic tripeptidomimetic scaffold through TFA-mediated cyclization of a linear precursor containing three side chains. The introduction of a triphenylmethyl-protected ...
    • Total Synthesis of Phorbazole B 

      Guttormsen, Yngve; Fairhurst, Magnus John Espeland; Pandey, Sunil Kumar; Isaksson, Johan; Haug, Bengt Erik; Bayer, Annette (Journal article; Peer reviewed, 2020)
      Phorbazoles are polychlorinated heterocyclic secondary metabolites isolated from a marine sponge and several of these natural products have shown inhibitory activity against cancer cells. In this work, a synthesis of the ...
    • Unequivocal structure confirmation of a breitfussin analog by anisotropic NMR measurements 

      Ndukwe, Ikenna E.; Lam, Yu-hong; Pandey, Sunil Kumar; Haug, Bengt Erik; Bayer, Annette; Sherer, Edward C.; Blinov, Kirill A.; Williamson, R. Thomas; Isaksson, Johan; Reibarkh, Mikhail; Liu, Yizhou; Martin, Gary E. (Journal article; Peer reviewed, 2020)
      Structural features of proton-deficient heteroaromatic natural products, such as the breitfussins, can severely complicate their characterization by NMR spectroscopy. For the breitfussins in particular, the constitution ...