One of the research lines developed at LaSOM is the synthesis of dihydropyrimidin-2-thiones (DHPMs) derivatives reported in the literature as antitumor agents due to kinesin Eg5 inhibition, which is present in the cell division process. The purpose of the study developed in this article was to test 19 DHPMs (including monastrol as reference) with N1 of the central ring replaced with a substituted-phenyl group against two cancer cell lines: U138 (glioblastoma) and T24 (bladder cancer). Based on the results generated, a quantitative structure-activity relationship study (QSAR) was prepared in order to identify the essential characteristics responsible for antitumor activity. In addition, the toxicity of the compounds with the most active profiles were evaluated in an alternative in vivo model Caenorhabditis elegans .

          The study was developed in partnership with Laboratory 22 of the Departamento de Bioquímica of the Instituto de Ciências Básicas da Saúde and with the Laboratório de Toxicologia (LATOX) - both are part of UFRGS. You can find the link for the article by clicking here. Nice reading!