Design, synthesize and evaluate De Novo anticancer agents with oxime and methyloxime containing anthraquinone derivatives.

• Main Authors: Chen,Cing-Hua, 陳慶樺
• Other Authors: Wang,Tai-Chi
• Format: Others
• Language: zh-TW
• Published: 2019
• Online Access: http://ndltd.ncl.edu.tw/handle/x94e34

碩士 === 大仁科技大學 === 藥學系碩士班 === 107 === Anthraquinone compounds, anthracyclines and anthracenediones, have long been used as effective anticancer drugs against a broad spectrum of tumors. Recently, we have prepared oxime and methyloxime-containing anthraquinone derivatives and evaluated in vitro for their anti-proliferative activities against a panel of human cancer cell lines including nasopharyngeal (NPC-TW01), lung carcinoma (NCI-H266), leukemia (Molt4), lymphoid (Sup-T1) and prostate adenocarcinoma (PC-3). Among them, methyloxime-containing anthraquinone derivatives exhibited active against NCI-H266, Molt4 and Sup-T1 with IC50 values less than 10 M. On the other hand, Oxime-containing anthraquinone derivatives are not shows significant cytotoxicity for five cell lines. In continuation of our studies to explore active and anti-cancer agents and establish structure-activity relationships. This study describes the preparation and anti-proliferative evaluation of oxime-containing anthraquinone derivatives and compares them with the activity of methyloxime-containing anthraquinone derivatives.