文献类型：期刊文献

英文题名：Rationally Designed Multitarget Anticancer Agents

作者：Chen, Zhuo[1];Han, Le[1];Xu, Minghao[1];Xu, Yufang[1];Qian, Xuhong[1]

机构：[1]E China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai Key Lab Chem Biol, Shanghai Key Lab New Drug Design,Sch Pharm, Shanghai 200237, Peoples R China

年份：2013

卷号：20

期号：13

起止页码：1694

外文期刊名：CURRENT MEDICINAL CHEMISTRY

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000316854600009)】；

基金：This work is financially supported by the National Basic Research Program of China (973 Program, 2010CB126100), the National High Technology Research and Development Program of China (863 Program 2011AA10A207), the China 111 Project (grant B07023), the Shanghai Leading Academic Discipline Project (B507), the Fundamental Research Funds for the Central Universities and the Shanghai Committee of Science and Technology [grant 11DZ2260600].

语种：英文

外文关键词：Multitarget; tumor; pharmacophore combination; quinazoline; naphthalimide; chemotherapy

摘要：Balanced modulation of multiple targets is an attractive therapeutic strategy in treating complex diseases including cancer. Comparing with drugs combination, single molecule modulating desirable multiple targets has advantages in pharmacokinetic and pharmacodynamics. Different from previous reviews, we provided an overview of reported multitarget antitumor agents from the viewpoint of pharmacophores. These multitarget antitumor agents were designed by combination of pharmacophores or by high-throughput screening plus structural modification, which were exemplified by the privileged pharmacophore quinazoline and several other popular pharmacophores, including phenylaminopyrimidine, anthracycline and naphthalimide. Previous research demonstrated the importance of in-depth validation against multiple targets not only in cell-free system, but also in cancer cells. Furthermore, the multitarget compounds were also effective for resistance cell lines which highlighted their antitumor potency in the era of increasing drug resistance in cancer patients.