Synthesis of Phenoxazinone Derivatives and Antiproliferative Activities on Wild-type and Drug-resistant Tumor Cells  

作　　者：Ji Wu RUAN Zhi Shu HUANG Jin Feng HUANG Cui Juan DU Shi Liang HUANG Zhi SHI Li Wu FU Lian Quan GU 

机构地区：[1]School of Pharmaceutical Sciences, Zhongshan University, Guangzhou 510080 [2]Cancer Center, Sun Yet-sen UniVersity, Guangziaou 510060

出　　处：《Chinese Chemical Letters》2006年第9期1141-1144,共4页中国化学快报（英文版）

基　　金：support by the National Natural Science Foundation of China(No.20472117);the Science Foundation of Zhuhai(PC20041131);the Scientific Research Foundation for the Returned 0verseas Chinese Scholars.

摘　　要：A series of novel phenoxazinone derivatives （1-6） were designed and synthesized for evaluating their antitumor activities. The antiproliferative activities of the prepared compounds against representative human neoplastic cell lines were evaluated by MTF assay. The results showed that most of them inhibited cell proliferation in a submicromolar to rnicromolar range. These compounds were also evaluated against KBv200 and MCF-7/Adr cell lines, which overexpress the MDR/P-glycoprotein drug efflux pump responsible for drug resistance, and had a more potential for resisting MDR than their lead compound APO.A series of novel phenoxazinone derivatives （1-6） were designed and synthesized for evaluating their antitumor activities. The antiproliferative activities of the prepared compounds against representative human neoplastic cell lines were evaluated by MTF assay. The results showed that most of them inhibited cell proliferation in a submicromolar to rnicromolar range. These compounds were also evaluated against KBv200 and MCF-7/Adr cell lines, which overexpress the MDR/P-glycoprotein drug efflux pump responsible for drug resistance, and had a more potential for resisting MDR than their lead compound APO.

关 键 词：ANTITUMOR phenoxazinones iminoquinones multidrug-resistance. 

分 类 号：R979.1[医药卫生—药品]