- Synthesis and biological evaluation of novel rhodanine-based structures with antiviral activity towards HHV-6 virus
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An increased awareness of diseases associated with Human herpesvirus 6 (HHV-6) infection or reactivation has resulted in a growing interest in the evaluation of the best treatment options available for the clinical management of HHV-6 disease. However, no
- Gentili, Valentina,Turrin, Giulia,Marchetti, Paolo,Rizzo, Sabrina,Schiuma, Giovanna,Beltrami, Silvia,Cristofori, Virginia,Illuminati, Davide,Compagnin, Greta,Trapella, Claudio,Rizzo, Roberta,Bortolotti, Daria,Fantinati, Anna
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- Rhodanine derivatives as potent anti-HIV and anti-HSV microbicides
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Although highly active antiretroviral therapies (HAART) remarkably increased life expectancy of HIV positive people, the rate of novel HIV-1 infections worldwide still represent a major concern. In this context, pre-exposure prophylaxis (PrEP) approaches
- Tintori, Cristina,Iovenitti, Giulia,Ceresola, Elisa Rita,Ferrarese, Roberto,Zamperini, Claudio,Brai, Annalaura,Poli, Giulio,Dreassi, Elena,Cagno, Valeria,Lembo, David,Canducci, Filippo,Botta, Maurizio
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- Novel broad spectrum virucidal molecules against enveloped viruses
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Viral infections are an important cause of death worldwide. Unfortunately, there is still a lack of antiviral drugs or vaccines for a large number of viruses, and this represents a remarkable challenge particularly for emerging and re-emerging viruses. For this reason, the identification of broad spectrum antiviral compounds provides a valuable opportunity for developing efficient antiviral therapies. Here we report on a class of rhodanine and thiobarbituric derivatives displaying a broad spectrum antiviral activity against seven different enveloped viruses including an HSV-2 acyclovir resistant strain with favorable selectivity indexes. Due to their selective action on enveloped viruses and to their lipid oxidation ability, we hypothesize a mechanism on the viral envelope that affects the fluidity of the lipid bilayer, thus compromising the efficiency of virus-cell fusion and preventing viral entry.
- Cagno, Valeria,Tintori, Cristina,Civra, Andrea,Cavalli, Roberta,Tiberi, Marika,Botta, Lorenzo,Brai, Annalaura,Poli, Giulio,Tapparel, Caroline,Lembo, David,Botta, Maurizio
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- One drug for two targets: Biological evaluation of antiretroviral agents endowed with antiproliferative activity
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AIDS-related cancer diseases are malignancies with low incidence on healthy people that affect mostly subjects already immunocompromised. The connection between HIV/AIDS and these cancers has not been established yet, but a weakened immune system is certa
- Botta, Lorenzo,Maccari, Giorgio,Calandro, Pierpaolo,Tiberi, Marika,Brai, Annalaura,Zamperini, Claudio,Canducci, Filippo,Chiariello, Mario,Martí-Centelles, Rosa,Falomir, Eva,Carda, Miguel
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supporting information
p. 2502 - 2505
(2017/05/09)
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- 2-Aminothiazolones as anti-hiv agents that act as gp120-cd4 inhibitors
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We report here the synthesis of 2-Aminothiazolones along with their biological properties as novel anti-HIV agents. Such compounds have proven to act through the inhibition of the gp120-CD4 protein-protein interaction that occurs at the very early stage of the HIV-1 entry process. No cytotoxicity was found for these compounds, and broad antiviral activities against laboratory strains and pseudotyped viruses were documented. Docking simulations have also been applied to predict the mechanism, at the molecular level, by which the inhibitors were able to interact within the Phe43 cavity of HIV-1 gp120. Furthermore, a preliminary absorption, distribution, metabolism, and excretion (ADME) evaluation was performed. Overall, this study led the basis for the development of more potent HIV entry inhibitors.
- Tiberi, Marika,Tintori, Cristina,Ceresola, Elisa Rita,Fazi, Roberta,Zamperini, Claudio,Calandro, Pierpaolo,Franchi, Luigi,Selvaraj, Manikandan,Botta, Lorenzo,Sampaolo, Michela,Saita, Diego,Ferrarese, Roberto,Clementi, Massimo,Canducci, Filippo,Botta, Maurizio
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supporting information
p. 3043 - 3052
(2014/06/09)
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- A Versatile and Practical Synthesis toward the Development of Novel HIV-1 Integrase Inhibitors
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As a continuation of our previous work, which resulted in the identification of a new hit compound as an HIV-1 integrase inhibitor, three novel series of salicylic acid derivatives were synthesized using three versatile and practical synthetic strategies and were assayed for their capacity to inhibit the catalytic activity of HIV-1 integrase. Biological evaluations revealed that some of the synthesized compounds possess good inhibitory potency in enzymatic assays and are able to inhibit viral replication in MT-4 cells at low micromolar concentrations. Finally, docking studies were conducted to analyze the binding mode of the synthesized compounds within the DNA binding site of integrase in order to refine their structure-activity relationships. Easy as A, B, C: Three new series of salicylic acid derivatives were designed and synthesized to investigate their activity toward HIV-1 integrase. Some of these compounds were obtained with microwave-assisted procedures developed and optimized in our research group, which allowed us to rapidly generate several final compounds of high purity.
- Rinaldi, Marta,Tintori, Cristina,Franchi, Luigi,Vignaroli, Giulia,Innitzer, Anna,Massa, Silvio,Este, Jose A.,Gonzalo, Encarna,Christ, Frauke,Debyser, Zeger,Botta, Maurizio
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experimental part
p. 343 - 352
(2012/01/11)
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- Exploration of novel thiobarbituric acid-, rhodanine- and thiohydantoin-based HIV-1 integrase inhibitors
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A novel compound inhibiting HIV-1 integrase has been identified by means of virtual screening techniques. A small family of structurally related molecules has been synthesized and biologically evaluated with some of the compounds possessing micromolar act
- Rajamaki, Suvi,Innitzer, Anna,Falciani, Chiara,Tintori, Cristina,Christ, Frauke,Witvrouw, Myriam,Debyser, Zeger,Massa, Silvio,Botta, Maurizio
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scheme or table
p. 3615 - 3618
(2010/03/31)
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