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首页> 外文期刊>Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents >Syntheses and in vitro biological screening of l-aryl-10H-[1,2,4]triazolo[3', 4':3, 4][1, 2, 4]triazino [5, 6-b]indoles
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Syntheses and in vitro biological screening of l-aryl-10H-[1,2,4]triazolo[3', 4':3, 4][1, 2, 4]triazino [5, 6-b]indoles

机译：1-芳基-10H- [1,2,4]三唑[3'，4'：3，4] [1,2,4]三嗪[5，6-b]吲哚的合成及体外生物学筛选

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摘要

Structurally diverse l-aryl-10H-[l,2,4]triazol-o[3',4':3,4][l,2,4]triazino[5,6-b]indoles 4a-v were synthesized by regiospecific heterocyclizations. The designed molecular diversity was evaluated in vitro in parallel cell-based assays for cytotoxicity of viruses multiplication supporting cell lines and antiviral activity against viruses representative of two of three genera of the Flaviviridae family. The compound library was also tested against Retrovirus (HIV-1), two Picornaviruses (CVB-2 and Sb-1), and Paramyxoviridae (VSV) representative. Among double-stranded RNA (dsRNA) viruses, Reoviridae representative (Reo-1) was tested. Two representatives of DNA virus families were also included-HSV-1 (Herpesviridae) and VV (Poxviridae). The compounds 4m and 4o were found cytotoxic, having CC50 values ranging from 4 to 30 uM. Moreover, compound 4v has exhibited significant activity (EC50 = 3 muM) against BVDV.
机译：合成结构上不同的l-芳基-10H- [1,2,4]三唑-o [3'，4'：3,4] [l，2,4]三嗪基[5,6-b]吲哚4a-v通过区域特异性杂环化。在基于平行细胞的实验中评估了设计的分子多样性，以评估支持细胞系的病毒繁殖的细胞毒性和对代表黄病毒科三个属中两个属的病毒的抗病毒活性。还针对逆转录病毒（HIV-1），两种小核糖核酸病毒（CVB-2和Sb-1）和副粘病毒科（VSV）代表测试了该化合物文库。在双链RNA（dsRNA）病毒中，测试了呼肠孤病毒科代表病毒（Reo-1）。 DNA病毒家族的两个代表还包括-HSV-1（疱疹病毒科）和VV（痘病毒科）。发现化合物4m和4o具有细胞毒性，CC50值为4至30 uM。此外，化合物4v对BVDV表现出显着的活性（EC50 = 3μM）。

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