Molecules, Vol. 28, Pages 6696: Antiviral Effect of 5 & prime;-Arylchalcogeno-3-aminothymidine Derivatives in SARS-CoV-2 Infection

Molecules, Vol. 28, Pages 6696: Antiviral Effect of 5′-Arylchalcogeno-3-aminothymidine Derivatives in SARS-CoV-2 Infection Molecules doi: 10.3390/molecules28186696 Authors: Amanda Resende Tucci Raquel Mello da Rosa Alice Santos Rosa Otávio Augusto Chaves Vivian Neuza Santos Ferreira Thamara Kelcya Fonseca Oliveira Daniel Dias Coutinho Souza Nathalia Roberto Resende Borba Luciano Dornelles Nayra Salazar Rocha João Candido Pilar Mayer João B. Teixeira da Rocha Oscar Endrigo D. Rodrigues Milene Dias Miranda The understanding that zidovudine (ZDV or azidothymidine, AZT) inhibits the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2 and that chalcogen atoms can increase the bioactivity and reduce the toxicity of AZT has directed our search for the discovery of novel potential anti-coronavirus compounds. Here, the antiviral activity of selenium and tellurium containing AZT derivatives in human type II pneumocytes cell model (Calu-3) and monkey kidney cells (Vero E6) infected with SARS-CoV-2, and their toxic effects on these cells, was evaluated. Cell viability analysis revealed that organoselenium (R3a–R3e) showed lower cytotoxicity than organotellurium (R3f, R3n–R3q), with CC50 ≥ 100 µM. The R3b and R3e were particularly noteworthy for inhibiting viral replication in both cell models and showed better selectivity index. In Vero E6, the EC50 values for R3b and R3e were 2.97 &...
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research