Abstract
A small library of analogues of annonaceous acetogenins through click linkage with aromatic moieties is established using a convergent modular fragment-assembly approach. These analogues exhibited low micromolar inhibitory activities against the proliferation of several human cancer cell lines. Structure-activity relationship (SAR) of these analogues indicates that replacement of the methoxy groups of ubiquinone ring with methyl groups is proved to be a useful strategy for improving the anticancer activity of quinone-acetogenin hybrids.
Original language | English (US) |
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Pages (from-to) | 248-258 |
Number of pages | 11 |
Journal | European Journal of Medicinal Chemistry |
Volume | 78 |
DOIs | |
State | Published - May 6 2014 |
Keywords
- Annonaceous acetogenins
- Aromatic functionalities
- Click chemistry
- Cytotoxicity
- Quinone
ASJC Scopus subject areas
- Drug Discovery
- Organic Chemistry
- Pharmacology