Synthesis, cytotoxicity, and DNA-topoisomerase inhibitory activity of new asymmetric ureas and thioureas |
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Authors: | Esteves-Souza Andressa Pissinate Kenia Nascimento Maria da Graça Grynberg Noema Faiga Echevarria Aurea |
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Affiliation: | Universidade Federal Rural do Rio de Janeiro, Seropédica, 23851-970, RJ, Brazil. |
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Abstract: | A new series of N-3,3-diphenylpropyl-N-(p-X-benzyl)-N'-phenylureas (5a-g) and thioureas (6a-g) were synthesized by the reaction of secondary amines and phenyl isocyanate or isothiocyanate. The cytotoxic effects of the urea and thiourea derivatives were evaluated by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay against Ehrlich carcinoma and K562 human leukemia cells. Moreover, the activity of compounds in the inhibition of DNA topoisomerases I and II-alpha was tested. The results indicated that the compounds presented important and promising antiproliferative action. |
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