Syntheses and in vitro biological screening of 1-aryl-10H-[1,2,4]triazolo[3′,4′:3,4][1,2,4]triazino[5,6-b]indoles

Structurally diverse 1-aryl-10 H -[1,2,4]triazolo[3′,4′:3,4][1,2,4]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 li...

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Bibliographic Details
Published in:Medicinal chemistry research 2013, Vol.22 (8), p.3675-3686
Main Authors: Upadhyay, Kuldip, Manvar, Atul, Loddo, Roberta, Colla, Paolo La, Virsodiya, Vijay, Trivedi, Jalpa, Chaniyara, Ravi, Shah, Anamik
Format: Article
Language:English
Subjects:
Antiviral activity
Aromatic compounds
Biochemistry
Biomedical and Life Sciences
Biomedicine
Cell Biology
Cell lines
Cytotoxicity
DNA viruses
Double-stranded RNA
HIV
Human immunodeficiency virus
Indoles
Multiplication
Original Research
Pharmacology/Toxicology
RNA viruses
Toxicity
Viruses
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Summary:Structurally diverse 1-aryl-10 H -[1,2,4]triazolo[3′,4′:3,4][1,2,4]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 CC 50 values ranging from 4 to 30 μM. Moreover, compound 4v has exhibited significant activity (EC 50  = 3 μM) against BVDV.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-012-0342-1