合成新型环丙沙星类似物及其对人癌细胞系抗增殖活性的评价。
Synthesis of novel ciprofloxacin analogues and evaluation of their anti-proliferative effect on human cancer cell lines.
机构信息
Department of Chemistry, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, Andhra Pradesh, India.
出版信息
Bioorg Med Chem Lett. 2013 Dec 1;23(23):6292-5. doi: 10.1016/j.bmcl.2013.09.077. Epub 2013 Oct 1.
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 ((1)H NMR, (13)C 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.
已经合成了一系列 22 种新型的 1-环丙基-6-氟-4-氧代-7-(4-取代哌嗪-1-基)-1,4-二氢喹啉-3-羧酸类似物，并对其进行了特征描述（1H NMR、13C NMR 和 LCMS），并评估了它们对人白血球急性淋巴母细胞（CCRF-CEM）、乳腺腺癌（MDA-MB-468）和人结肠癌细胞（HCT-116）增殖的抑制活性。在所合成的所有环丙沙星类似物中，3t 在 50μM 时在所有三种细胞系中的活性与多柔比星（10μM）相当，而 3j 对 MDA-MB-468 的增殖抑制作用选择性高达 35%，优于其他两种细胞系。
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