Abstract
In prosecution of an anti-Flaviviridae project a new series of variously substituted 2-diphenyl-benzimidazoles were synthesized and tested in vitro for antiviral and antiproliferative activities. Compounds were tested in cell-based assays against viruses representative of: i) two of the three genera of the Flaviviridae family, i.e. Flaviviruses and Pestiviruses; ii) other RNA virus families, such as Retroviridae, Picornaviridae, Paramyxoviridae, Rhabdoviridae and Reoviridae; iii) two DNA virus families (Herpesviridae and Poxviridae). The 5- Acetyl-2-(4-nitrobiphenyl-4-yl)-1H-benzimidazole (24) emerged as potent active lead compound against Yellow Fever Virus (a Flavivirus) (EC50= 0.5 μM) and CVB-2 at 1 μM and was not cytotoxic, whereas the other title benzimidazoles showed no antiviral activity at concentrations not cytotoxic for the resting cell monolayers. Among the examined series, the most cytotoxic derivatives (11,12,14,16,18,19,20,21,23,25-30) against mock-infected MT-4 cells (CC50 < 8.0 μM) were evaluated against a panel of human cell lines derived from haematological and solid tumours, using 6-mercaptopurine (6-MP) and etoposide as reference drugs. In particular, compounds 26 and 28 showed a similar potency of 6-MP and etoposide.
Keywords: 2-Arylbenzimidazoles, Antiviral, antiproliferative activities, Flaviviridae, Retroviridae, Poxviridae
Medicinal Chemistry
Title: 2-Arylbenzimidazoles as Antiviral and Antiproliferative Agents-Part 2
Volume: 5 Issue: 6
Author(s): Gabriella Vitale, Paola Corona, Mario Loriga, Antonio Carta, Giuseppe Paglietti, Paolo La Colla, Bernardetta Busonera, Esther Marongiu, David Collu and Roberta Loddo
Affiliation:
Keywords: 2-Arylbenzimidazoles, Antiviral, antiproliferative activities, Flaviviridae, Retroviridae, Poxviridae
Abstract: In prosecution of an anti-Flaviviridae project a new series of variously substituted 2-diphenyl-benzimidazoles were synthesized and tested in vitro for antiviral and antiproliferative activities. Compounds were tested in cell-based assays against viruses representative of: i) two of the three genera of the Flaviviridae family, i.e. Flaviviruses and Pestiviruses; ii) other RNA virus families, such as Retroviridae, Picornaviridae, Paramyxoviridae, Rhabdoviridae and Reoviridae; iii) two DNA virus families (Herpesviridae and Poxviridae). The 5- Acetyl-2-(4-nitrobiphenyl-4-yl)-1H-benzimidazole (24) emerged as potent active lead compound against Yellow Fever Virus (a Flavivirus) (EC50= 0.5 μM) and CVB-2 at 1 μM and was not cytotoxic, whereas the other title benzimidazoles showed no antiviral activity at concentrations not cytotoxic for the resting cell monolayers. Among the examined series, the most cytotoxic derivatives (11,12,14,16,18,19,20,21,23,25-30) against mock-infected MT-4 cells (CC50 < 8.0 μM) were evaluated against a panel of human cell lines derived from haematological and solid tumours, using 6-mercaptopurine (6-MP) and etoposide as reference drugs. In particular, compounds 26 and 28 showed a similar potency of 6-MP and etoposide.
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Vitale Gabriella, Corona Paola, Loriga Mario, Carta Antonio, Paglietti Giuseppe, Colla La Paolo, Busonera Bernardetta, Marongiu Esther, Collu David and Loddo Roberta, 2-Arylbenzimidazoles as Antiviral and Antiproliferative Agents-Part 2, Medicinal Chemistry 2009; 5 (6) . https://dx.doi.org/10.2174/157340609790170542
DOI https://dx.doi.org/10.2174/157340609790170542 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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