Asymmetric Total Synthesis and Absolute Stereochemistry of the Neuroactive Marine Macrolide Palmyrolide A

The first asymmetric total synthesis and determination of the absolute configuration for the neuroactive marine macrolide palmyrolide A is described. The highlight of the synthesis is macrocyclization <i>via trans</i>-enamide formation catalyzed by copper(I) iodide and cesium carbonate. Comparison with the authentic spectral data confirms the synthesis of (+)-<i>ent</i>-palmyrolide A

Cystargolide-based amide and ester Pz analogues as proteasome inhibitors and anti-cancer agents

A series of cystargolide-based β-lactone analogues containing nitrogen atoms at the Pz portion of the scaffold were prepared and evaluated as proteasome inhibitors, and for their cytotoxicity profile toward several cancer cell lines. Inclusion of one, two or even three nitrogen atoms at the Pz portion of the cystargolide scaffold is well tolerated, producing analogues with low nanomolar proteasome inhibition activity, in many cases superior to carfilzomib. Additionally, analogue 8g, containing an ester and pyrazine group at Pz, was shown to possess significant activity toward RPMI 8226 cells (IC50 = 21 nM) and to be less cytotoxic toward the normal tissue model MCF10A cells than carfilzomib

Big data analysis for drilling and blasting in a mine in the central andes

Big Data applied to mining, contemplates the combination of algorithms located in advanced technological tools to process a quantity of data, Power BI allows the interaction of different data formats, for integration it has the support of Python Script. In this article, Big Data was applied to essential activities such as drilling and blasting, analyzing the parameters, standards, quantities, advances, the objective was to develop an integration system of a quantity of data for its analysis and interpretation, it will contribute to decision making in the mining operation. The development of Dashboard for interactive reportability based on indicators, will allow to visualize more efficiently and in a virtual way among the interested parties. Finally, the application of Big Data in the field of mining mainly in the treatment of its data will be the trend of the future which will allow to optimize the time and the functionality of the reports

Bicyclic Cyclohexenones as Inhibitors of NF-κB Signaling

A series of structurally simplified cryptocaryone analogues were synthesized by a facile Pd-catalyzed acetoxylation of alkyne-tethered cyclohexadienones and evaluated as inhibitors of NF-κB signaling. Compounds <b>10</b> and <b>11</b> were found to possess low micromolar inhibitory properties toward induced NF-κB activity by blocking p50/p65 nuclear protein through a covalent inhibition mechanism. Both compounds were able to inhibit NF-κB-induced IL-8 expression and exhibited antiproliferative activity against two model cancer cell lines. These analogues constitute a promising new scaffold for the development of novel NF-κB inhibitors and anticancer agents