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首页> 外文期刊>Archiv der Pharmazie >Synthesis and biological evaluation of some polymethoxylated fused pyridine ring systems as antitumor agents.
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Synthesis and biological evaluation of some polymethoxylated fused pyridine ring systems as antitumor agents.

机译：一些抗肿瘤药物的聚甲氧基化吡啶环系统的合成和生物学评估。

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A series of 3,5-bis(arylidene)-4-piperidones like chalcone analogues carrying variety of methoxylated aryl groups, pyrazolo[4,3-c]pyridines, pyrido[4,3-d]pyrimidines, and pyrido[3,2-c]pyridines, carrying an arylidene moiety, and some pyrano[3,2-c]pyridines, like flavone and coumarin isosteres, were synthesized and screened for their in-vitro antitumor activity at the National Cancer Institute (NCI, USA). The tested compounds 7, 9, 10, 12, 13, 15, 17, and 19 exhibited a broad spectrum of antitumor activity. Compounds belonging to the pyrazolo[4,3-c]pyridine series proved to be more active than those of the pyrido[3,2-c]pyridine and pyrano[3,2-c]pyridine analogues, in which the monomethoxylated derivatives showed better antitumor activity when compared with their corresponding dimethoxylated congeners. Compound 7 is considered to be the most active member identified in this study with a broad spectrum of activity against 22 different tumor cell lines belonging to the nine subpanels employed, and a particular effectiveness against the breast cancer T-47D cell line (GI 54.7%). The pyrano[3,2-c]pyridine heterocyclic system 19 proved to be the most active antitumor agent among the six-membered fused pyridines, with variable activity against 18 different tumor cell lines, and special activity against the non-small cell lung cancer Hop-92 and ovarian cancer OVCAR-4 cell lines (GI values 63.9 and 48.5%, respectively).
机译：一系列3,5-双（亚芳基）-4-哌啶酮，如查尔酮类似物，带有各种甲氧基化的芳基，吡唑并[4,3-c]吡啶，吡啶并[4,3-d]嘧啶和吡啶并[3，合成了带有亚芳基部分的2-c]吡啶和一些吡喃并[3,2-c]吡啶，如黄酮和香豆素等位基因，并在美国国家癌症研究所（NCI）进行了体外抗肿瘤活性的筛选。被测试的化合物7、9、10、12、13、15、17和19表现出广谱的抗肿瘤活性。吡唑并[4,3-c]吡啶系列化合物被证明比吡啶并[3,2-c]吡啶和吡喃并[3,2-c]吡啶类似物具有更高的活性，其中单甲氧基化衍生物显示出与它们相应的二甲氧基化同类物相比，具有更好的抗肿瘤活性。化合物7被认为是本研究中最活跃的成员，具有针对属于所使用的9个子面板的22种不同肿瘤细胞系的广谱活性，并且对乳腺癌T-47D细胞系具有特殊的功效（GI 54.7％） ）。吡喃并[3,2-c]吡啶杂环系统19被证明是六元稠合吡啶中最活跃的抗肿瘤药物，对18种不同的肿瘤细胞系具有可变的活性，对非小细胞肺癌具有特殊的活性。 Hop-92和卵巢癌OVCAR-4细胞系（GI值分别为63.9和48.5％）。

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