Identification of a diverse synthetic abietane diterpenoid library for anticancer activity

  • Bioorg Med Chem Lett. 2017 Feb 1;27(3):505-510. doi: 10.1016/j.bmcl.2016.12.032.
Hongtao Xu  1 ,  Lili Liu  2 ,  Xiaoting Fan  3 ,  Guanjun Zhang  4 ,  Yuanchao Li  5 ,  Biao Jiang  6
Affiliations
  • 1. Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, Shanghai 201210, PR China; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, PR China.
  • 2. Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, Shanghai 201210, PR China.
  • 3. Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, Shanghai 201210, PR China; Institute of Biochemistry and Cell Biology, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200031, PR China.
  • 4. College of Chemical Engineering and Materials Science, Tianjin University of Science & Technology, Tianjin 300457, PR China.
  • 5. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, PR China.
  • 6. Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, Shanghai 201210, PR China. Electronic address: [email protected].
PMID: 28011223 DOI: 10.1016/j.bmcl.2016.12.032
Abstract

A diverse natural-product-like synthetic abietane diterpenoid library contains about 56 compounds were obtained, and evaluated for their potential in vitro cytotoxic or antitumor activity against A549, PC-3 and SKOV-3 tumor cell lines by SRB assay. Treatment of A549 cells with the most potent compound ketone 19 showed induction of Apoptosis, as revealed by JC-1 mitochondrial membrane potential staining, TUNNEL assay, western blotting analysis and flow cytometry assay.

Keywords
Abietic acid; Anticancer; Diverse; Natural-product-like; Triptophenolide.