Synthesis and antitumor evaluation of desmosdumotin C derivatives on B-ring / 中国药学杂志

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.