Please use this identifier to cite or link to this item:
http://dx.doi.org/10.25673/37399
Title: | Novel nonsymmetrical 1,4-dihydropyridines as inhibitors of nonsymmetrical MRP-efflux pumps for anticancer therapy |
Author(s): | Kreutzer, David Ritter, Christoph Hilgeroth, Andreas |
Issue Date: | 2020 |
Type: | Article |
Language: | English |
Abstract: | Cancer is a strong global burden with increasing numbers of diseases and ongoing anticancer drug resistance. The number of structurally novel anticancer drugs is strongly limited. They cause high costs for the social health systems. Most critical so-called multidrug resistances (MDR) are caused by transmembrane efflux pumps that transport drugs with various structures out of the cancer cells. Multidrug resistance proteins (MRPs) type 1 and 2 are found overexpressed in various kinds of cancer. There is a strong need for inhibitors of those efflux pumps. We developed novel nonsymmetrical 1,4-dihydropyridines as novel inhibitors of cancer relevant MRP types 1 and 2. The structure-dependent activities of the differently substituted derivatives were evaluated in cellular assays of respective cancer cells and are discussed. Promising candidates were identified. One candidate was demonstrated to resensitize a cisplatin resistant cancer cell line and thus to overcome the anticancer drug resistance. |
URI: | https://opendata.uni-halle.de//handle/1981185920/37642 http://dx.doi.org/10.25673/37399 |
Open Access: | Open access publication |
License: | (CC BY 4.0) Creative Commons Attribution 4.0 |
Sponsor/Funder: | Publikationsfond MLU |
Journal Title: | Pharmaceuticals |
Publisher: | MDPI |
Publisher Place: | Basel |
Volume: | 13 |
Issue: | 7 |
Original Publication: | 10.3390/ph13070146 |
Appears in Collections: | Open Access Publikationen der MLU |
Files in This Item:
File | Description | Size | Format | |
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pharmaceuticals-13-00146-v2.pdf | 405.06 kB | Adobe PDF | View/Open |