@misc{10498/30042, year = {2023}, month = {5}, url = {http://hdl.handle.net/10498/30042}, abstract = {Naphthoquinones are a valuable source of secondary metabolites that are well known for their dye properties since ancient times. A wide range of biological activities have been described highlighting their cytotoxic activity, gaining the attention of researchers in recent years. In addition, it is also worth mentioning that many anticancer drugs possess a naphthoquinone backbone in their structure. Considering this background, the work described herein reports the evaluation of the cytotoxicity of different acyl and alkyl derivatives from juglone and lawsone that showed the best activity results from a etiolated wheat coleoptile bioassay. This bioassay is rapid, highly sensitive to a wide spectrum of activities, and is a powerful tool for detecting biologically active natural products. A preliminary cell viability bioassay was performed on cervix carcinoma (HeLa) cells for 24 h. The most promising compounds were further tested for apoptosis on different tumoral (IGROV-1 and SK-MEL-28) and non-tumoral (HEK-293) cell lines by flow cytometry. Results reveal that derivatives from lawsone (particularly derivative 4) were more cytotoxic on tumoral than in non-tumoral cells, showing similar results to those obtained with of etoposide, which is used as a positive control for apoptotic cell death. These findings encourage further studies on the development of new anticancer drugs for more directed therapies and reduced side effects with naphthoquinone skeleton.}, publisher = {MDPI}, keywords = {naphthoquinones}, keywords = {cytotoxic activity}, keywords = {juglone}, keywords = {lawsone}, keywords = {flow cytometry}, title = {Biological Activity of Naphthoquinones Derivatives in the Search of Anticancer Lead Compounds}, doi = {10.3390/toxins15050348}, author = {García Durán, Alexandra and Chinchilla Salcedo, Nuria and Simonet Morales, Ana María and Gutiérrez Amares, María Teresa and Bolívar Pérez, Jorge and Martínez Valdivia, Manuel Jesús and González Molinillo, José María and Macías Domínguez, Francisco Antonio}, }