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Discovery of cytochrome bc(1) complex inhibitors inspired by the natural product karrikinolide

机译：发现细胞色素BC（1）由天然产物Karrikinolide的复杂抑制剂

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摘要

The cytochrome bc(1) complex (cyt bc(1) or complex III) is a promising target of numerous antibiotics and fungicides. With an aim to indentify new lead structures for the bc(1) complex, a series of novel inhibitors were discovered from the natural product karrikinolide for the first time. Extensive screening results suggested variable inhibitory activities of these compounds against succinate-cytochrome reductase [SCR, a mixture of respiratory complex II (SQR) and complex III (the bc(1) complex)], implying the essential role of a 4-substituted phenyl group for the high potency. Exceptionally, compound 12g showed excellent inhibition potency having an IC50 value in the sub-micromolar range, demonstrating its higher potency than the commercial control amisulbrom by over two orders of magnitude. Further experiments inferred that these newly prepared compounds mainly target the bc(1) complex. Seemingly, this work has presented a new lead scaffold for further development of bc(1) complex inhibitors.
机译：细胞色素BC（1）复合物（CYT BC（1）或复合物III）是许多抗生素和杀真菌剂有希望的靶点。以目标indentify新的先导结构的BC（1）配合物，一系列新的抑制剂被从天然产物karrikinolide首次发现的。广泛的筛选结果表明针对琥珀酸 - 细胞色素还原酶[SCR，呼吸复合物II（SQR）和复合物III（的BC（1）配合物）的混合物中这些化合物的可变抑制活性，这意味着一个4-取代的苯基的重要作用组的高效力。特殊情况下，化合物显示出12克中具有亚微摩尔范围的IC 50值优良抑制效力，通过在两个数量级的展示其比商用控制吲唑磺更高的效力。进一步的实验推断，这些新制备的化合物主要靶向BC（1）复合物。表面上看，这项工作提出了（1）复合物抑制剂的BC进一步发展新的领导支架。

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  • 来源
    《RSC Advances》 |2016年第100期|共7页
  • 作者

    Chen Cheng; Wu Qiong-You; Shan Lian-Ying; Zhang Bei; Verpoort Francis; Yang Guang-Fu;

  • 作者单位

    Wuhan Univ Technol State Key Lab Adv Technol Mat Synth &

    Proc Wuhan 430070 Peoples R China;

    Cent China Normal Univ Coll Chem Key Lab Pesticide &

    Chem Biol Wuhan 430079 Peoples R China;

    Cent China Normal Univ Coll Chem Key Lab Pesticide &

    Chem Biol Wuhan 430079 Peoples R China;

    Cent China Normal Univ Coll Chem Key Lab Pesticide &

    Chem Biol Wuhan 430079 Peoples R China;

    Wuhan Univ Technol State Key Lab Adv Technol Mat Synth &

    Proc Wuhan 430070 Peoples R China;

    Cent China Normal Univ Coll Chem Key Lab Pesticide &

    Chem Biol Wuhan 430079 Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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