Synthesis and cytotoxic activity evaluation of 8-substituted quercetin derivatives / 国际药学研究杂志

ABSTRACT

Objective: To synthesize 8-substituted quercetin derivatives and test their cytotoxicity on human cancer cell lines, so as to find out hit or lead compounds via structure activity relationship(SAR)analysis. Methods: Using rutin as the raw material, quercetin was obtained by the acid hydrolysis of rutin, and the 8-substituted quercetin derivatives, 3a-3h, were synthesized via the whole hydroxyl protection of quercetin and then halogenation, followed by the Suzuki coupling or heck coupling reaction. The in vitro inhibitory activity of these derivatives was assayed by the MTT method using human cancer HepG2, HT-29 and K562 cell lines. Results and Conclusion: Eight new target compounds, 3a-3h, were synthesized, and their structures were confirmed by the 1H NMR, 13C NMR and MS data. The inhibitory effect of 3b-3h on HepG2 cell line, 3b and 3d on HT-29 cell line, and 3b-3d and 3f-3h on K562 cell line has remarkably and significantly enhanced than that of quercetin, and the present research results provide a suggestive preliminary SAR.