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首页> 外文期刊>Archiv der Pharmazie >Synthesis and in vitro Anticancer Activities of some Selenadiazole Derivatives
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Synthesis and in vitro Anticancer Activities of some Selenadiazole Derivatives

机译：硒代二唑衍生物的合成及体外抗癌活性

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摘要

A novel series of fourteen substituted selenadiazoles has been synthesized and the compounds tested for their in vitro antiproliferative and cytotoxic activities. The tests were carried out against leukemia (CCRF-CEM), colon (HT-29), lung (HTB-54), and breast (MCF-7) cancer cells. In order to assess the selectivity of the compounds under investigation the assays were also carried out on two non-tumoral lines – one mammary (184B5) and one bronchial epithelium (BEAS-2B) cell line. Assay-based antiproliferative activity studies revealed that seven derivatives (2a, 2c, 2e, 2f, 2g, 3a, and 3b) exhibited good activity against MCF-7 cells: for instance, 2c and 2f inhibited cell growth with nanomolar GI50 values. Compound 2f had a better antitumoral profile than vinorelbine and paclitaxel, two drugs that are used as first-line treatments in advanced, recurrent, and/or metastatic cancer. In the other cell lines the compounds showed moderate activity or were inactive – with the exception of 2a, which was also found to have antiproliferative activity. Modulation of the cell cycle and apoptotic effects of active compounds were further evaluated in MCF-7 cells. Of these, 6-bromo[1,2,5]selenadiazolo[3,4-b]pyridine (2a) was the most active, with an apoptogenic effect 3.9 times higher than that of camptothecin, which was used as a positive control. Compound 2a also provoked cell cycle arrest with a significant decrease in the G0/G1 phase cell population and an increase in S and G2/M cells, thus suggesting mitotic arrest prior to metaphase.
机译：已经合成了一系列新的十四个取代的硒代二唑，并测试了这些化合物的体外抗增殖和细胞毒性活性。测试针对白血病（CCRF-CEM），结肠（HT-29），肺癌（HTB-54）和乳腺癌（MCF-7）癌细胞进行。为了评估所研究化合物的选择性，还对两种非肿瘤细胞系进行了测定-一种是乳腺（184B5），另一种是支气管上皮细胞（BEAS-2B）。基于分析的抗增殖活性研究表明，七种衍生物（2a，2c，2e，2f，2g，3a和3b）表现出对MCF-7细胞的良好活性：例如，2c和2f抑制了纳摩尔GI的细胞生长。 50个值。化合物2f具有比长春瑞滨和紫杉醇更好的抗肿瘤特性，长春瑞滨和紫杉醇是在晚期，复发和/或转移性癌症中用作一线治疗的两种药物。在其他细胞系中，化合物显示中等活性或无活性-2a除外，后者也被发现具有抗增殖活性。在MCF-7细胞中进一步评估了细胞周期的调节和活性化合物的凋亡作用。其中，6-溴[1,2,5]硒二氮杂[3,4-b]吡啶（2a）最活跃，其凋亡作用是喜树碱的3.9倍，后者被用作阳性对照。化合物2a还引起细胞周期停滞，G 0 / G 1 期细胞群显着减少，而S和G 2 增加/ M细胞，因此提示在中期之前有丝分裂停滞。

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  • 来源
    《Archiv der Pharmazie》 |2010年第12期|p.680-691|共12页
  • 作者

    Daniel Plano; Esther Moreno; María Font; Ignacio Encío; Juan Antonio Palop; Carmen Sanmartín;

  • 作者单位

    Sección de Síntesis, Departamento de Química Orgánica y Farmacéutica, University of Navarra, Pamplona, Spain;

    Sección de Síntesis, Departamento de Química Orgánica y Farmacéutica, University of Navarra, Pamplona, Spain;

    Sección de Modelización Molecular, Departamento de Química Orgánica y Farmacéutica, University of Navarra, Pamplona, Spain;

    Departamento de Ciencias de la Salud, Universidad Pública de Navarra, Pamplona, Spain;

    Sección de Síntesis, Departamento de Química Orgánica y Farmacéutica, University of Navarra, Pamplona, Spain;

    Sección de Síntesis, Departamento de Química Orgánica y Farmacéutica, University of Navarra, Pamplona, Spain;

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  • 关键词

    Antitumorals; Apoptosis; Cytotoxics; Selenadiazoles; Selenium;

    机译：抗肿瘤;细胞凋亡;细胞毒素;硒代二唑;硒;

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