Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 30, Issue 22, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2020.127522
Keywords
Piperazine; Histamine H-3 receptor ligands; Cancer; Antiproliferative; MDR efflux pumps; ABCB1; T-Lymphoma
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Funding
- National Science Center, Poland [2016/23/N/NZ7/00469]
- Jagiellonian Interdisciplinary PhD Programme
- Polish Statutory Research Project [N42/DBS/000027]
- COST [CA15135, CA18133]
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Taking into account that multidrug resistance (MDR) is the main cause for chemotherapeutic failure in cancer treatment, the ability of novel histamine H-3 receptor ligands to reverse the cancer MDR was evaluated, using the ABCB1 efflux pump inhibition assay in mouse MDR T-lymphoma cells. The most active compounds displayed significant cytotoxic and antiproliferative effects as well as a very potent MDR efflux pump inhibitory action, 3-5-fold stronger than that of reference inhibitor verapamil. Although these compounds possess weak antagonistic properties against histamine H-3 receptors, they are valuable pharmacological tools in the search for novel anticancer molecules. Furthermore, for the most active compounds, an insight into mechanisms of action using either, the luminescent Pgp-GloTM Assay in vitro or docking studies to human Pgp, was performed.
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