Taking into account that multidrug resistance (MDR) is the main cause for chemotherapeutic failure in cancer treatment, the ability of novel histamine H₃ 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 H₃ 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-Glo™ Assay in vitro or docking studies to human Pgp, was performed.

考虑到多药耐药性（MDR）是癌症治疗中化疗失败的主要原因，因此在小鼠MDR T淋巴瘤中使用ABCB1外排泵抑制试验评估了新型组胺H ₃受体配体逆转癌症MDR的能力。细胞。活性最高的化合物显示出显着的细胞毒性和抗增殖作用，以及非常有效的MDR外排泵抑制作用，比参考抑制剂维拉帕米强3至5倍。尽管这些化合物对组胺H ₃具有弱的拮抗特性受体，它们是寻找新型抗癌分子的有价值的药理工具。此外，对于活性最高的化合物，使用发光Pgp-Glo™体外测定法或与人Pgp的对接研究对作用机理进行了深入研究。