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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Rationally Designed Multitarget Anticancer Agents

Author(s): Zhuo Chen, Le Han, Minghao Xu, Yufang Xu and Xuhong Qian

Volume 20 , Issue 13 , 2013

Page: [1694 - 1714] Pages: 21

DOI: 10.2174/0929867311320130009

Price: $65


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.

Keywords: Multitarget, tumor, pharmacophore combination, quinazoline, naphthalimide, chemotherapy

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