Abstract
Abstract Multidrug resistance (MDR) of cancer cells is a major cause of therapeutic failure. One of the mechanisms of MDR is the overexpression of efflux pump such as ABCB1. The use of ABCB1 inhibitors constitute an important strategy for reversing MDR. Thus, this study aimed to synthesize a novel 2-oxo-1,2-dihydroquinoline-4-carboxylic acid derivatives and evaluate their biological activities in vitro using parental (PAR) and multidrug resistant (MDR; ABCB1-overexpressing) mouse T-lymphoma cells. The cytotoxic activity and selectivity of the tested compounds were assessed by MTT method. The ABCB1 modulating activity was measured by rhodamine 123 accumulation assay using flow cytometry. The results showed that the compounds 2b, 2c and 3b exerted cytotoxic activity with IC50MDR value of 9.09 μM, 71.14 μM and 19.09 μM, respectively. The most active compound 8c should be considered as a lead compound for further derivatization and additional biological assays.
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