American Chemical Society
np5b00774_si_001.pdf (557.11 kB)

Cytotoxic Evaluation against Breast Cancer Cells of Isoliquiritigenin Analogues from Spatholobus suberectus and Their Synthetic Derivatives

Download (557.11 kB)
journal contribution
posted on 2016-01-22, 00:00 authored by Fu Peng, Chun-Wang Meng, Qin-Mei Zhou, Jian-Ping Chen, Liang Xiong
Five isoliquiritigenin analogues, including a new methylene-bridged bischalcone (1), were isolated from Spatholobus suberectus. Cytotoxicity screening of these isolates and several synthetic derivatives indicated that the introduction, removal, position modification, or glycosylation of hydroxy groups in isoliquiritigenin did not improve the resultant cytotoxicity against the MCF-7 and MDA-MB-231 human breast cancer cell lines. In addition, cyclization of OH-2′ chalcones or reduction of the α,β-unsaturated carbonyl double bond decreased such cytotoxicity substantially. However, methylation of hydroxy groups resulted in a marked increase in such cytotoxic activity. Among these active isoliquiritigenin analogues, 3′,4′,5′,4″-tetramethoxychalcone (3h) was obtained as a compound with promising cytotoxic activity.