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Esters of bendamustine are by far more potent cytotoxic agents than the parent compound against human sarcoma and carcinoma cells

Huber, Stefan, Huettner, Johannes Philip, Kristina, Hacker, Bernhardt, Günther, König, Jörg and Buschauer, Armin (2015) Esters of bendamustine are by far more potent cytotoxic agents than the parent compound against human sarcoma and carcinoma cells. PLoS One 10 (7), PLoSe0133743.

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Date of publication of this fulltext: 09 Jul 2015 08:11

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Abstract

The alkylating agent bendamustine is approved for the treatment of hematopoietic malignancies such as non-Hodgkin lymphoma, chronic lymphocytic leukemia and multiple myeloma. As preliminary data on recently disclosed bendamustine esters suggested increased cytotoxicity, we investigated representative derivatives in more detail. Especially basic esters, which are positively charged under ...

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Item type:Article
Date:2015
Additional Information (public):Supporting Information on Methods and 16 Supplementary Figures available.
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Chemistry and Pharmacy > Institute of Pharmacy > Pharmacology and Toxicology (Prof. Schlossmann, formerly Prof. Seifert)
Projects:Open Access Publizieren (DFG)
Identification Number:
ValueType
10.1371/journal.pone.0133743DOI
26196503PubMed ID
Related URLs:
URLURL Type
http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0133743Publisher
Keywords:Bendamustine;bendamustine ester;N-lost;nitrogen mustard;alkylating agent;chemosensitivity;cytotoxic;kinetic cytotoxicity assay;Apoptosis;p53;tumor suppressor;propidium iodide;Annexin V;sarcoma cells;carcinoma cells;organic cation transporter;OCT1;SLC22A1;OCT3;SLC22A3;HEK-OCT1 cells;HEK-OCT3 cells;Flow cytometry;Confocal Microscopy;[3H]MPP+;ASP+ uptake;SK-MEL-3;malignant melanoma;Capan-1;Pancreatic adenocarcinoma;HT-29;colorectal adenocarcinoma;SK-ES-1;Ewing´s sarcoma;HEL92.1.7;erythroleukemia;Jurkat;acute T-cell leukemia;U-937;histiocytic lymphoma;LNCaP;prostate cancer;NCI-H460;large cell lung cancer;MG-63;osteosarcoma;HEK293;HaCaT cells;spontaneously immortalized keratinocytes;preferential cytotoxicity
Dewey Decimal Classification:600 Technology > 615 Pharmacy
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Item ID:31238
Owner only: item control page

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