Synthesis and uptake of fluorescence-labeled Combi-molecules by P-glycoprotein-proficient and-deficient uterine sarcoma cells MES-SA and MES-SA/DX5

AL Larroque-Lombard, M Todorova…

Index: Larroque-Lombard, Anne-Laure; Todorova, Margarita; Golabi, Nahid; Williams, Christopher; Jean-Claude, Bertrand J. Journal of Medicinal Chemistry, 2010 , vol. 53, # 5 p. 2104 - 2113

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Citation Number: 8

Abstract

Here, we report on the first synthesis of fluorescent-labeled epidermal growth factor receptor− DNA targeting combi-molecules, and we studied the influence of P-glycoprotein status of human sarcoma MES-SA cells on their growth inhibitory effect and cellular uptake. The results showed that 6, bearing a longer spacer between the quinazoline ring and the dansyl group, was more stable and more cytotoxic than 4. In contrast to the latter, it ...