
Effect of N-1 arylation of monastrol on kinesin Eg5 inhibition in glioma cell lines
2018; Royal Society of Chemistry; Volume: 9; Issue: 6 Linguagem: Inglês
10.1039/c8md00095f
ISSN2040-2511
AutoresItamar Luís Gonçalves, Liliana Rockenbach, Gustavo Machado das Neves, Gabriela Göethel, Fabiana Nascimento, Luciano Porto Kagami, Fabrício Figueiró, Gabriel Oliveira de Azambuja, Amanda de Fraga Dias, A Benitez Amaro, Lauro Mera de Souza, Ivan da Rocha Pitta, Daiana Silva Ávila, Daniel Fábio Kawano, Solange Cristina García, Ana Maria Oliveira Battastini, Vera Lucia Eifler‐Lima,
Tópico(s)Advanced Fluorescence Microscopy Techniques
ResumoAn original and focused library of two sets of dihydropyrimidin-2-thiones (DHPMs) substituted with N-1 aryl groups derived from monastrol was designed and synthesized in order to discover a more effective Eg5 ligand than the template. Based on molecular docking studies, four ligands were selected to perform pharmacological investigations against two glioma cell lines. The results led to the discovery of two original compounds, called
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