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Synthesis of Novel 1,3-Diacetoxy-Acridones as Cytotoxic Agents and their DNA-Binding Studies

机译：新型1,3-二乙酰氧基-rid啶酮作为细胞毒剂的合成及其DNA结合研究

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A series of novel substituted acridones (1-15) have been synthesized. Their in vitro cytotoxicity against human breast adenocarcinoma (MCF-7) and human promyelocytic leukemia (HL-60) cell lines has been investigated. The compounds 11, 12, 14 and 15 showed moderate activity against MCF-7 cell lines with IC_(50) value < 5.83 μM. The compounds 8, 10-12, and 15 showed moderate activity against HL-60 cell lines with IC50 value < 1.75 μM. The DNA-binding properties of the compounds were evaluated based on their affinity or intercalation with CT-DNA measured with absorption titration. The compound 12 bearing planar diacetoxy tricyclic ring linked with butyl piperidine side chain showed highest binding affinity with binding constant (Ki) 10.38 ×10 × M~(-1)The examination of the relationship between lipophilicity and cytotoxic properties of acridones showed a poor correlation.
机译：已经合成了一系列新颖的取代的cri啶酮（1-15）。研究了它们对人乳腺腺癌（MCF-7）和人早幼粒细胞白血病（HL-60）细胞系的体外细胞毒性。化合物11、12、14和15对MCF-7细胞系显示中等活性，IC_（50）值<5.83μM。化合物8、10-12和15对HL-60细胞系显示中等活性，IC50值<1.75μM。基于它们的亲和力或通过吸收滴定测量的与CT-DNA的插入，评估化合物的DNA结合特性。与丁基哌啶侧链连接的带有平面二乙酰氧基三环的化合物12表现出最高的结合亲和力，结合常数（Ki）为10.38×10×M〜（-1）。对丙烯酰胺的亲脂性与细胞毒性性质之间的关系进行的研究表明相关性较弱。

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