Mild Pd-Catalyzed Aminocarbonylation of (Hetero)Aryl Bromides with a Palladacycle Precatalyst

A palladacyclic precatalyst is employed to cleanly generate a highly active XantPhos-ligated Pd-catalyst. Its use in low temperature aminocarbonylations of (hetero)aryl bromides provides access to a range of challenging products in good to excellent yields with low catalyst loading and only a slight excess of CO. Some products are unattainable by traditional carbonylative coupling.National Institutes of Health (U.S.) (Award GM46059)Danish National Research Foundation (Grant DNRF59)Villum FoundationDanish Council for Independent Researc

New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer

We synthesized 3-aroyl-1-arylpyrrole (ARAP) derivatives as potential anticancer agents having different substituents at the pendant 1-phenyl ring. Both the 1-phenyl ring and 3-(3,4,5-trimethoxyphenyl)carbonyl moieties were mandatory to achieve potent inhibition of tubulin polymerization, binding of colchicine to tubulin, and cancer cell growth. ARAP 22 showed strong inhibition of the P-glycoprotein-overexpressing NCI-ADR-RES and Messa/Dx5MDR cell lines. Compounds 22 and 27 suppressed in vitro the Hedgehog signaling pathway, strongly reducing luciferase activity in SAG treated NIH3T3 Shh-Light II cells, and inhibited the growth of medulloblastoma D283 cells at nanomolar concentrations. ARAPs 22 and 27 represent a new potent class of tubulin polymerization and cancer cell growth inhibitors with the potential to inhibit the Hedgehog signaling pathway

Data for: Syntheses of o-iodobenzyl alcohols‒BODIPY structures as potential bimodal tags for positron emission tomography and optical imaging.

Spectra of absorbance / emission, and determination of the quantum yields for [13C]6, [13C]14 and [13C]24. 1H and 13C NMR spectra of new compounds

Data for: Syntheses of o-iodobenzyl alcohols‒BODIPY structures as potential bimodal tags for positron emission tomography and optical imaging.

Spectra of absorbance / emission, and determination of the quantum yields for [13C]6, [13C]14 and [13C]24. 1H and 13C NMR spectra of new compounds

Modélisation mathématique de l'hématopoïèse et des hémopathies : développement, dynamique et traitement

National audienceL'étude de l'hématopoïèse normale et pathologique, de par la complexité du sujet, requiert une approche multi-disciplinaire. L'utilisation de modèles mathématiques, lorsqu'il s'agit de comprendre la dynamique de populations de cellules, le développement de cancers ou l'effet d'un traitement, est particulièrement appropriée. Les modèles mathématiques, calibrés à partir d'observations expérimentales, peuvent être des outils d'aide à la décision en clinique, permettant par exemple de prédire l'effet d'un traitement ou d'en optimiser le dosage. Dans cette revue, nous commencerons par présenter différents modèles et formalismes mathématiques qui se sont développés au cours des décennies pour modéliser l'hématopoïèse, et qui sont encore pour certains à la base des travaux les plus récents. Nous aborderons ensuite les enjeux méthodologiques liés à l'inférence mathématique, permettant de s'assurer de la validité et robustesse des résultats. Enfin, nous terminerons par illustrer l'utilisation de modèles mathématiques dans trois champs d'application : l'initiation et le développement des hémopathies malignes, la dérégulation de leur hématopoïèse et leurs traitements

X-ray absorption spectroscopy investigations on radioactive matter using MARS beamline at SOLEIL synchrotron

International audienceThe MARS beamline at the SOLEIL synchrotron is dedicated to the characterization of radioactive material samples. One great advantage of the beamline is the possibility to characterize about 380 radionuclides by different X-ray techniques in the same place. This facility is unique in Europe. A wide energy range from around 3.5 keV to 36 keV K-edges from K to Cs, and L3 edges from Cd to Am and beyond can be used. The MARS beamline is optimized for X-ray absorption spectroscopy techniques (XANES/EXAFS), powder diffraction (XRD) but x-ray fluorescence (XRF) analysis, High Energy Resolution Fluorescence Detected -XAS (HERFD-XAS), X-ray Emission (XES) and μ-XAS/XRD are also possible. A description of the beamline as well as its performances are given in a first part. Then some scientific examples of XAS studies from users are presented which cover a wide variety of topics in radiochemistry and nuclear materials