The AAPS Journal

, 11:435 | Cite as

Structure–Activity Relationships of Tariquidar Analogs as Multidrug Resistance Modulators

  • Ilza K. Pajeva
  • Michael WieseEmail author
Review Article Theme: Structure-Activity Relationships for ABC Transporters


The review summarizes the most recent achievements in structure–activity relationship (SAR) studies of tariquidar and its analogs. Tariquidar is one of the most promising representatives of the third generation of multidrug resistance (MDR) modulators created so far. This fact determines the strong interest of different research groups in the development of tariquidar-like structures as selective inhibitors of MDR transporters in resistant human cancer cells. After the discovery of tariquidar, a number of analogs have been synthesized and pharmacologically tested, thus supplying good data for comprehensive analyses of their structure–activity relationships. In the review, the structural and pharmacological data of newly synthesized tariquidar-like compounds are first presented. Next, the main achievements in the SAR studies are described focusing on two main transport proteins: P-glycoprotein and breast cancer resistance protein. The reported results are discussed from the point of view of their significance and importance for future directions in the rational design of effective MDR modulators.

Key words

BCRP modeling multidrug resistance pharmacophore P-glycoprotein QSAR 



We thank our colleagues and especially Christoph Globisch, Werner Klinkammer, and Henrik Müller whose efforts contributed to our results and knowledge on the topic. The financial support from the Alexander von Humboldt Foundation and Deutsche Forschungsgemeinschaft is also highly recognized.


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Copyright information

© American Association of Pharmaceutical Scientists 2009

Authors and Affiliations

  1. 1.Centre of Biomedical EngineeringBulgarian Academy of ScienceSofiaBulgaria
  2. 2.Pharmaceutical Chemistry II, Pharmaceutical InstituteUniversity of BonnBonnGermany

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