title: Rationally designed multitarget anticancer agents.
abstract: 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.
authors: State Key Laboratory of Bioreactor Engineering, Shanghai Key Laboratory of Chemical Biology, Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
authors: Zhuo
authors: Z
authors: Chen
authors: Le
authors: L
authors: Han
authors: Minghao
authors: M
authors: Xu
authors: Yufang
authors: Y
authors: Xu
authors: Xuhong
authors: X
authors: Qian
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D058990:Molecular Targeted Therapy / Q000379:methods; D053644:Naphthalimides / Q000737:chemistry* / Q000494:pharmacology; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D011799:Quinazolines / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D053644:Naphthalimides; D011799:Quinazolines