1404305-73-2Relevant academic research and scientific papers
Discovery, synthesis and biological evaluation of cycloprotoberberine derivatives as potential antitumor agents
Li, Yang-Biao,Zhao, Wu-Li,Wang, Yan-Xiang,Zhang, Cai-Xia,Jiang, Jian-Dong,Bi, Chong-Wen,Tang, Sheng,Chen, Ru-Xian,Shao, Rong-Guang,Song, Dan-Qing
, p. 463 - 472 (2013/10/01)
A series of new 1,13-cycloprotoberberine derivatives defined through variations at the 9-position were designed, synthesized and evaluated for their cytotoxicities in human HepG2 (hepatoma), HT1080 (fibrosarcoma) and HCT116 (colon cancer) cells. The preliminary structure-activity relationship (SAR) revealed that the replacement of 9-methoxyl with an ester moiety might significantly enhance the antiproliferative activity in vitro. Notably, compound 7f demonstrated equipotent cytotoxicity activity against breast cancer MCF-7 (parent) and doxorubicin (DOX)-resistant MCF-7 (MCF-7/ADrR) cells, indicating a mode of action different from that of DOX. Further mechanism study showed that 7f significantly inhibited activity of DNA topoisomerase I (Top I) and Top II. G2/M phase arrest and tumor cell growth reduction was observed thereafter. Thus, we consider cycloprotoberberine analogues to be a new family of promising antitumor agents with an advantage of inhibiting drug-resistant cancer cells.
