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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

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

Volume 11, Issue 7, 2011

Page: [611 - 624] Pages: 14

DOI: 10.2174/138955711795906923

Price: $65


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.

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

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