Synthesis and biological evaluation of new antiseizure compounds derived from valproic acid

This article focuses on the design of new anticonvulsant compounds that combine the chemical structure of valproic acid with other interesting scaffolds with anticonvulsant or anti-inflammatory properties. These compounds protected against in vivo acute seizure models (mice). The results revealed the capacity of combining known scaffolds into a single structure to generate new active compounds with multitarget purposes.Facultad de Ciencias ExactasUniversidad de Buenos AiresLaboratorio de Investigación y Desarrollo de Bioactivo

β-Lapachone analogs with enhanced antiproliferative activity

In this study, we describe the synthesis of a series of α- and β-lapachone containing hydroxyl or methoxyl groups on the benzene ring, by means of the selective acid promoted cyclization of the appropriate lapachol analog. The evaluation of the antiproliferative activity in human solid tumor cell lines provided 7-hydroxy-β-lapachone as lead with enhanced activity over the parent drug β-lapachone. Cell cycle studies, protein expression experiments, and reactive oxygen species analysis revealed that, similarly to β-lapachone, ROS formation and DNA damage are critical factors in the cellular toxicity of 7-hydroxy-β-lapachone.Co-financed by the European Social Fund (FEDER), the Spanish Instituto de Salud Carlos III (PI11/00840), the Spanish MSC (RTICC RD06/0020/1046 and RD06/0020/0041), the Canary Islands ACIISI (PI 2007/021), the Canary Islands FUNCIS (PI 43/ 09), and by the Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET PIP 0447), and Universidad de Buenos Aires (UBACyT 20020090200697). E.L.B. thanks CONICET for a fellowship. L.G.L. thanks ACIISI for a postdoctoral contract (SE- 10/19).Peer Reviewe

Versatile Supramolecular Organogel with Outstanding Stability toward Aqueous Interfaces

In this communication, we report on a novel and versatile low-molecular-weight organogelator. The methanolic gel exhibits an exceptional water-enhanced stability as evidenced by a 30 °C increase in <i>T</i>_g with up to 10%v/v of water. This atypical property not observed with other solvents makes of this supramolecular gel a highly stable matrix compatible with aqueous interfaces. As a proof of principle we present the sensing performance of a symmetric tricarbocyanine fluorophore bearing a Zn­(II)­chelator unit. The system retained its remarkable physical integrity for a long period of time opening new possibilities for other organic–aqueous interface applications