Ultrasonic imaging using conditional generative adversarial networks.

The Full Matrix Capture (FMC) and Total Focusing Method (TFM) combination is often considered the gold standard in ultrasonic nondestructive testing, however it may be impractical due to the amount of time required to gather and process the FMC, particularly for high cadence inspections. This study proposes replacing conventional FMC acquisition and TFM processing with a single zero-degree plane wave (PW) insonification and a conditional Generative Adversarial Network (cGAN) trained to produce TFM-like images. Three models with different cGAN architectures and loss formulations were tested in different scenarios.

Hemisynthetic alkaloids derived from trilobine are antimalarials with sustained activity in multidrug-resistant .

Malaria eradication requires the development of new drugs to combat drug-resistant parasites. We identified bisbenzylisoquinoline alkaloids isolated from that are active against blood stages. Synthesis of a library of 94 hemi-synthetic derivatives allowed to identify compound that kills multi-drug resistant clinical isolates in the nanomolar range (median IC ranging from 35 to 88 nM).

Design and synthesis of new non nucleoside inhibitors of DNMT3A.

DNA methylation, an epigenetic modification regulating gene expression, is a promising target in cancer. In an effort to identify new non nucleosidic inhibitors of DNA methyltransferases, the enzymes responsible for DNA methylation, we carried out a high-throughput screening of 66,000 chemical compounds based on an enzymatic assay against catalytic DNMT3A. A family of propiophenone derivatives was identified.

Anticancer activity of koningic acid and semisynthetic derivatives.

A screening program aimed at discovering novel anticancer agents based on natural products led to the selection of koningic acid (KA), known as a potent inhibitor of glycolysis. A method was set up to produce this fungal sesquiterpene lactone in large quantities by fermentation, thus allowing (i) an extensive analysis of its anticancer potential in vitro and in vivo and (ii) the semi-synthesis of analogues to delineate structure-activity relationships. KA was characterized as a potent, but non-selective cytotoxic agent, active under both normoxic and hypoxic conditions and inactive in the A549 lung cancer xenograft model.

Anthranilic acid derivatives and other components from Ononis pusilla.

Three new anthranilic acid derivatives: N-(R)-3'-hydroxydocosanoylanthranilic acid (1), N-(R)-3'-hydroxytricosanoylanthranilic acid (2) and N-(R)-3'-hydroxytetracosanoylanthranilic acid (3), in addition to one knownanthranilic acid and six known flavonoids, were isolated from the ethyl acetate extract of Ononis pusilla L. The structures of the isolated compounds were assigned by spectroscopic methods, including 1D and 2D homo and heteronuclear NMR experiments, ESI-MS, chemical transformation and comparison with literature data.