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Synthesis and Antitumor Activity of Evil/Thiadiazole Fluoroquinolone Hydrazone Sulfides

Author: YinJun
Tutor: HuGuoQiang
School: Henan University
Course: Medicinal Chemistry
Keywords: quinolone aromatic heterocycle chloroacetaldehyde and antitumor activity
CLC: R96
Type: Master's thesis
Year: 2013
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In recent years, especially malignant tumor has become the number one killer of human health tumors,a serious impact on human life and quality of life. Currently on the market although there are manyantineoplastic agents, the role of these drugs mainly for cell division, the use of the process will affectnormal tissue cells, while killing malignant cells, but also some normal tissues also have a certain degree ofdamage, Therefore, the research and development of new structural efficiency and low toxicity ofanticancer drugs is particularly important. The quinolone is1,4-dihydro-4-oxo-3-quinoline carboxylicacid skeleton having a broad-spectrum antimicrobial activity of fully synthetic drugs, enzymescorresponding to the target because of its antibacterial action-topoisomerase mammal function andsequence similarity can be converted to its antimicrobial activity to the anti-tumor activity, the developmentof anti-cancer the quinolone become one of the focus of anticancer drugs.Currently, people focus on the structural modification of the quinolone compound in the quinoline ring,N-1and C-7, the modification of the structure of the other positions less. Recent studies indicate that theC-3carboxy group is not required a group of quinolone anti-tumor activity, may be substituted by its rowlooking for a conversion to the anti-tumor quinolone antibacterial carbostyril effective ways and means ofstructural modification.1.Design and Synthesis of target compoundsThe target compounds synthesized mainly by the following three components:①quinoloneC-3-carboxylic acid hydrazide synthesis, starting the original, the hydrazine hydrate reflux that was left/ofloxacin.②aromatic mercapto heterocyclic synthesis, aromatic formic acid as the starting material,esterification and hydrazinolysis with CS2pro-nuclear salt, then closed loop in the environment of the alkalineand acidic conditions, respectively corresponding mercapto oxadiazole and thiadiazole③chloroacetaldehydefor connecting "bridge" the ultimate synthesis of the objective compound to adopt a "one-pot" of the previoustwo steps resulting quinolone C-3carboxylic acid hydrazide, aromatic the mercapto heterocyclic,chloroacetaldehyde three stirred at room temperature i.e. final target product.The twenty new synthesis of target compounds was confirmed by ESI-MS,1H-NMR and IR spectra and those compounds were firstreported.2.In vitro anticancer activity evaluationUsing the MTT assay method evaluation of target compounds on human hepatoma SMMC-7721cells. in vitro growth inhibition vitro anti-tumor cell activity of research and analysis shows that:10μmol L-1concentrations of the synthesized compounds. SMMC-7721cell inhibition in vitro mostly more thancontroll (ofloxacin, levofloxacin), which YA5YB5, YB6, YB8inhibition rate reached58.48%,66.75%,51.48%,65.80%, respectively; IC509.4μmol L-1,8.6μmol L-1,8.7μmol L-1,9.4μmol L-1, respectively,showed potential anti-tumor activity.3.ConclusionDesigned and synthesized20new compounds of the structure of derivatives in vitro anti-tumor activityscreening showed that some of these compounds have good anti-tumor activity, with the value of furtherrstudy.

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