Mini-Reviews in Medicinal Chemistry


Strategies on the Development of Small Molecule Anticancer Drugs for Targeted Therapy

Author(s): Y.-H. Lu, X.-Q. Gao, M. Wu, D. Zhang-Negrerie and Q. Gao

Affiliation: Tianjin Key Laboratory for Modern Drug Delivery and High-Efficiency, School of Pharmaceutical Science and Technology, Tianjin University, P. R. China.

Keywords: Targeted therapy, anticancer, drug design, drug resistance, prodrug, transporter, conjugate, chemotherapy, cytostatic drugs, mechanisms, advantages, tumor targeting, ombi-targeting


The main challenges currently encountered in chemotherapy are the lack of tumor selectivity and drug resistance. The design of novel cytostatic drugs has become the state-of-the-art technology in terms of targeted tumor therapy. This review illustrates the mechanisms and the advantages of representative chemotherapeutic agents, and presents an updated summary of the various drug design strategies developed by modern medicinal chemists during the most recent tumor targeting research which include rational design for overcoming drug resistance, the combi-targeting strategy, the prodrug approach, and tumor specific transporter based drug design. The concept of transporter related tumor targeting strategies for small molecule anticancer drug design discussed in this review may be amenable to predictable drug discovery for targeted therapy.

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Article Details

Page: [611 - 624]
Pages: 14
DOI: 10.2174/138955711795906923