RT Conference Proceedings
T1 Synthesis and Biological Evaluation of Depudecin Analogues
A1 Cheng-Sánchez, Iván
A1 Carrillo Fernández, Paloma
A1 García-Ruiz, Cristina
A1 Martínez-Póveda, Beatriz Amparo
A1 Rodríguez-Quesada, Ana María
A1 Medina-Torres, Miguel Ángel
A1 Sarabia-García, Francisco Ramón
K1 Tumores - Crecimiento
K1 Cáncer - Tratamiento
AB (-)-Depudecin (1) (Figure 1), isolated from the culture broths of the fungus Alternaria brassicicola,1 and later, from the weed pathogen Nimbya scirpicola,2 has been identified as a selective inhibitor of histone deacetylases (HDAC) with an IC50 in the low M range.3 In contrast to representative HDAC inhibitors, depudecin represents a unique inhibitor of these enzymes by virtue of its molecular structure, featuring the presence of two oxirane rings separated by a trans double bond. Originally discovered as part of a biological screening directed towards the identification of antitumour agents with detransforming activity,4 depudecin was identified as a bioactive metabolite capable of reverting the transformed morphology of tumor cells. This biological activity elicited a great biomedical and biological interest by virtue of its potential as an antitumor agent as well as for further understanding the biological roles of HDACs. Depudecin induced not only morphological changes but also cell cycle arrest and cellular differentiation,5 and also exhibited remarkable anti-angiogenesis activity.6 Prompted by its striking biological properties and enticing structure, we decided to initiate a research program directed towards the synthesis of natural depudecin. Our synthetic plan has recently culminated with linear and convergent total syntheses.7
YR 2019
FD 2019-09-18
LK https://hdl.handle.net/10630/18378
UL https://hdl.handle.net/10630/18378
LA spa
NO Universidad de Málaga. Campus de Excelencia Internacional Andalucía Tech
DS RIUMA. Repositorio Institucional de la Universidad de Málaga
RD 21 ene 2026