Synthesis and antitumor evaluation of desmosdumotin C derivatives on B-ring
- Author:
En-Zhen LI
1
Author Information
- Publication Type:Journal Article
- Keywords: Antitumor evaluation in vitro; Desmosdumotin C derivatives; Synthesis
- From: Chinese Pharmaceutical Journal 2013;48(11):924-929
- CountryChina
- Language:Chinese
- Abstract: OBJECTIVE: To synthesize desmosdumotin C derivatives on B-ring with antitumor activity. METHODS: The target compounds were synthesized from 2, 4, 6-trihydroxyacetophenone via methylation, O-methylation and aldol reaction. Their antiproliferative activities were tested against six human tumor cell lines. RESULTS: Fourteen target compounds were synthesized, nine of which were new compounds. All of them were characterized using 1H-NMR, 13C-NMR and MS. CONCLUSION: Preliminary pharmacological test showed that all the title compounds except 1i exhibited potent antitumor activities. 1h and 1n were better than desmosdumotin C in vitro. Introducing two fluoro atom on B-ring would benefit its activity against some tumor cells.
