Identification of a diverse synthetic abietane diterpenoid library for anticancer activity

Hongtao Xu; Lili Liu; Xiaoting Fan; Guanjun Zhang; Yuanchao Li; Biao Jiang

doi:10.1016/j.bmcl.2016.12.032

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. Epub 2016 Dec 11.

Authors

Hongtao Xu¹, Lili Liu², Xiaoting Fan³, Guanjun Zhang⁴, Yuanchao Li⁵, Biao Jiang⁶

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: jiangbiao@shanghaitech.edu.cn.

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.

MeSH terms

Abietanes / chemical synthesis
Abietanes / chemistry
Abietanes / pharmacology*
Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Cell Line, Tumor
Cell Proliferation / drug effects
Cell Survival / drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Membrane Potential, Mitochondrial / drug effects
Molecular Structure
Structure-Activity Relationship

Substances

Abietanes
Antineoplastic Agents