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Synthesis of Novel Series of Phthalazine Derivatives as Potential Antitumor Agents

机译:新型邻苯二嗪衍生物作为潜在抗肿瘤药的合成

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摘要

A novel series of phthalazine derivatives bearing isoindol-1,3-dione moiety were synthesized by treating 2-[4-(4-chlorophthalazine-1-yl)phenyl]-1H-isoindole-1,3-(2H)-dione 3 with various chemical reagents.The newly synthesi- zed compounds were characterized on the basis of their spectral (1H NMR, 13C NMR, Ms, IR) analyses. In vitro, most of the synthesized derivatives were screened for their antitumor activity against HepG2 cells using MTT assay. Compounds 11, 18 and 19c showed the most potent cytotoxic effect concluded from their IC50 values 217.4, 240.3 and 234.5 μg/ml respectively.
机译:通过处理2- [4-(4-氯酞嗪-1-基)苯基] -1H-异吲哚-1,3-(2H)-二酮3合成一系列带有异吲哚-1,3-二酮部分的新型酞嗪衍生物。新合成的化合物根据其光谱(1H NMR,13C NMR,Ms,IR)分析进行表征。在体外,使用MTT分析法筛选了大多数合成衍生物对HepG2细胞的抗肿瘤活性。化合物11、18和19c的IC50值分别为217.4、240.3和234.5μg/ ml,显示出最有效的细胞毒性作用。

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