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DNA sequence-specific ligands. XVIII. Synthesis, physico-chemical properties; genetic, virological, and biochemical studies of fluorescent dimeric bisbenzimidazoles DBPA(n).
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2020-02-13 , DOI: 10.1016/j.bmc.2020.115378 Vasiliy S Koval 1 , Albert F Arutyunyan 1 , Victor I Salyanov 1 , Alexey A Kostyukov 2 , Olga E Melkina 3 , Gennadii B Zavilgelsky 3 , Regina R Klimova 4 , Alla A Kushch 4 , Sergey P Korolev 5 , Yulia Yu Agapkina 5 , Marina B Gottikh 5 , Andrey V Vaiman 6 , Ekaterina Yu Rybalkina 6 , Olga Yu Susova 6 , Alexei L Zhuze 1
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2020-02-13 , DOI: 10.1016/j.bmc.2020.115378 Vasiliy S Koval 1 , Albert F Arutyunyan 1 , Victor I Salyanov 1 , Alexey A Kostyukov 2 , Olga E Melkina 3 , Gennadii B Zavilgelsky 3 , Regina R Klimova 4 , Alla A Kushch 4 , Sergey P Korolev 5 , Yulia Yu Agapkina 5 , Marina B Gottikh 5 , Andrey V Vaiman 6 , Ekaterina Yu Rybalkina 6 , Olga Yu Susova 6 , Alexei L Zhuze 1
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A set of AT-specific fluorescent dimeric bisbenzimidazoles DBPA(n) with linkers of different lengths bound to DNA in the minor groove were synthesized and their genetic, virological, and biochemical studies were performed. The DBPA(n) were shown to be effective inhibitors of the histon-like protein H-NS, a regulator of the DNA transcription factor, as well as of the Aliivibrio logei Quorum Sensing regulatory system in E. coli cells. Their antiviral activity was tested in model cell lines infected with herpes simplex virus type I. Also, it was found that DBPA(n) could inhibit catalytic activities of HIV-1 integrase at low micromolar concentrations. All of the dimeric bisbenzimidazoles DBPA(n) manifested fluorescent properties, were well soluble in water, nontoxic up to concentrations of 200 µM, and could penetrate into nuclei followed by binding to DNA.
中文翻译：
DNA序列特异性配体。十八。合成，理化性质；荧光二聚双苯并咪唑类DBPA（n）的遗传，病毒学和生化研究。
合成了一组具有特定长度的接头的AT特异性荧光二聚双苯并咪唑DBPA（n），该接头与小沟中的DNA结合，并进行了遗传，病毒学和生化研究。DBPA（n）被证明是大肠杆菌细胞中组蛋白样蛋白H-NS（DNA转录因子的调节剂）以及对数Aliivibrio logei Quorum Sensing调节系统的有效抑制剂。在感染了I型单纯疱疹病毒的模型细胞系中测试了它们的抗病毒活性。此外，还发现DBPA（n）在低微摩尔浓度下可以抑制HIV-1整合酶的催化活性。所有的二聚双苯并咪唑DBPA（n）均具有荧光性质，可很好地溶于水，在200 µM的浓度下无毒，
更新日期：2020-02-20
中文翻译：
DNA序列特异性配体。十八。合成，理化性质；荧光二聚双苯并咪唑类DBPA（n）的遗传，病毒学和生化研究。
合成了一组具有特定长度的接头的AT特异性荧光二聚双苯并咪唑DBPA（n），该接头与小沟中的DNA结合，并进行了遗传，病毒学和生化研究。DBPA（n）被证明是大肠杆菌细胞中组蛋白样蛋白H-NS（DNA转录因子的调节剂）以及对数Aliivibrio logei Quorum Sensing调节系统的有效抑制剂。在感染了I型单纯疱疹病毒的模型细胞系中测试了它们的抗病毒活性。此外，还发现DBPA（n）在低微摩尔浓度下可以抑制HIV-1整合酶的催化活性。所有的二聚双苯并咪唑DBPA（n）均具有荧光性质，可很好地溶于水，在200 µM的浓度下无毒，
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