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Synthesis of novel ciprofloxacin analogues and evaluation of their anti-proliferative effect on human cancer cell lines

机译:新型环丙沙星类似物的合成及其对人癌细胞系抗增殖作用的评估

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摘要

A series of twenty two novel 1-cyclopropyl-6-fluoro-4-oxo-7-(4-substituted piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid analogues have been synthesized, characterized (1H NMR, 13C NMR and LCMS) and evaluated for their inhibitory activity on the proliferation of human caucasian acute lymphoblastic leukemia cells (CCRF-CEM), breast adenocarcinoma cells (MDA-MB-468) and human colon carcinoma cells (HCT-116). Among all the synthesized ciprofloxacin analogues 3t at 50 μM showed comparable potency to doxorubicin (10 μM) in all three cell lines and 3j inhibited proliferation of MDA-MB-468 up to 35% selectively over other two cell lines.
机译:合成了一系列22个新颖的1-环丙基-6-氟-4-氧代-7-(4-取代的哌嗪-1-基)-1,4-二氢喹啉-3-羧酸类似物,其特征在于(1H NMR ,13C NMR和LCMS),并评估其对人白种人急性淋巴细胞白血病细胞(CCRF-CEM),乳腺癌细胞(MDA-MB-468)和人结肠癌细胞(HCT-116)的抑制活性。在所有合成的环丙沙星类似物中,浓度为50μM的3t在所有三个细胞系中均表现出与阿霉素(10μM)相当的效力,并且3j选择性抑制MDA-MB-468的增殖,选择性超过其他两个细胞系35%。

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