2. Academic Validation
  3. Photo-induced synthesis of Axinastatin 3 analogs, the secondary structures and their in vitro antitumor activities

Photo-induced synthesis of Axinastatin 3 analogs, the secondary structures and their in vitro antitumor activities

  • Bioorg Med Chem Lett. 2019 Nov 15;29(22):126730. doi: 10.1016/j.bmcl.2019.126730.
Yujun Bao 1,  Lishuang Zhao 2,  Jingwan Wu 1,  Shitian Jiang 1,  Zhiqiang Wang 3,  Yingxue Jin 4
Affiliations

Affiliations

  • 1 Key Laboratory of Photochemistry Biomaterials and Energy Storage Materials of Heilongjiang Province, College of Chemistry & Chemical Engineering, Harbin Normal University, Harbin 150025, China.
  • 2 Key Laboratory of Molecular Cytogenetics and Genetic Breeding of Heilongjiang Province, Harbin, College of Life Science and Technology, Harbin Normal University, Harbin 150025, China.
  • 3 Key Laboratory of Photochemistry Biomaterials and Energy Storage Materials of Heilongjiang Province, College of Chemistry & Chemical Engineering, Harbin Normal University, Harbin 150025, China. Electronic address: wzq70402@163.com.
  • 4 Key Laboratory of Photochemistry Biomaterials and Energy Storage Materials of Heilongjiang Province, College of Chemistry & Chemical Engineering, Harbin Normal University, Harbin 150025, China. Electronic address: jyxprof@163.com.
PMID: 31607609 DOI: 10.1016/j.bmcl.2019.126730
Abstract

Cyclic Peptides combine several favorable properties such as good binding affinity, target selectivity and low toxicity that make them an attractive modality for drug development. In an effort to identify what conformation could be accounting for the bioactive disparity of natural and synthetic cyclic Peptides, some structurally-constrained analogs of cyclopeptide Axinastatin 3 were prepared by photo-induced single electron transfer (SET) reaction. Detailed stereochemistry study was performed by experimental electronic circular dichroism combined with theoretical calculations. Our study suggested that the cyclopeptide 1 with βI-turn presented stronger antitumor activity comparing with those without such secondary structures. Moreover, a rare 'π helix unit' (compound 3) was realized because of the constrained cyclic structure, which could be considered an important research object for future study of unique helix secondary structures.

Keywords

Antitumor activity; Cyclopeptide; Photo-induced; Synthesis.

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