Recent Advances in the Development of P-gp Inhibitors

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Recent Advances in the Development of P-gp Inhibitors

Anti-Cancer Agents in Medicinal Chemistry, 9(4): 415-436.

Author(s): Christiane Baumert and Andreas Hilgeroth.

Affiliation: Martin Luther University Halle-Wittenberg, Institute of Pharmacy, Wolfgang-Langenbeck-Strasse 4, 06120 Halle (Saale), Germany.


During the last decades multidrug resistance (MDR) emerged as main problem in the anti-cancer therapy with cytostatically active agents. Classical as well as recently developed cytostatics develop the phenomenon of loosing activity in former drug-sensitive cells. Although MDR is a multifactorial process, the main obstacle is the expression of multidrug-efflux pumps that lowers the intracellular drug levels. P-glycoprotein (P-gp) is the longest identified efflux pump. As the attempt to overcome MDR by the use of inhibitors of the efflux pump activities turned out as most promising effect, the development of P-gp inhibitors has been a challenge for medicinal chemists. The article reviews the advances in P-gp inhibitor development by focussing on structure-activity relationships in the different compound classes to document improvements. The success has been the reduction of cytotoxic properties. The undesired activities could be much lowered in the case of compound classes that were derived from pharmacologically active drugs. Undesired drug interactions and limited in vivo activities are still a problem.


Multidrug resistance, P-gp inhibitor, development.

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Article Details

Volume: 9
Issue Number: 4
First Page: 415
Last Page: 436
Page Count: 22
DOI: 10.2174/1871520610909040415
Price: $58

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