Design, synthesis, and cytotoxic activities of novel hybrids of parthenolide and thiazolidinedione via click chemistry

Abstract

A series of novel parthenolide–thiazolidinedione hybrids have been synthesized via a click chemistry-mediated coupling between parthenolide and thiazolidinedione, and evaluated for their cytotoxic activities. The results indicated that all the hybrids showed moderate cytotoxic effects on human cancer cell lines, including human erythroleukemia cell line (HEL), prostate (PC3), and breast (MDA-MB-231) by MTT assay. In particular, compound VI-6 exhibited the best cytotoxic activities against the MDA-MB-231 cells with IC₅₀ value of 2.07 µM, which was about eight times more active than that of the original compound (PTL). These interesting results might be used to develop novel lead scaffolds for potential anticancer agents.

Graphical Abstract

Keywords:

• Parthenolide–thiazolidinedione hybrids
• click chemistry
• cytotoxic activities

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This study was financially supported by the 100 Talented Leaders of Guizhou Province (fund for Xiaojiang Hao and Yanmei Li), the Science and Technology Project of Guizhou (QKH PTRC-2017-5737), the Science and Technology project of Guizhou (Grant No. QKHT Z-2014-4007), the Technology Plan of Guizhou (Grant No. QKH YSZ-2015-4009), and “Light of the West” Talent Cultivation Program of Chinese Academy of Sciences (201684).