15 research outputs found
Epothilones as Lead Structures for the Synthesis-Based Discovery of New Chemotypes for Microtubule Stabilization
Total Synthesis of Hypermodified Epothilone Analogs with Potent in Vitro Antitumor Activity
GOCE: The first seismometer in orbit around the Earth
The first in situ sounding of a post-seismic infrasound wavefront is presented, using data from the GOCE mission. The atmospheric infrasounds following the great Tohoku earthquake (on 11 March 2011) induce variations of air density and vertical acceleration of the GOCE platform. These signals are detected at two positions along the GOCE orbit corresponding to a crossing and a doubling of the infrasonic wavefront created by seismic surface waves. Perturbations up to 11% of air density and 1.35?×?10???7?m/s2 of vertical acceleration are observed and modeled with two different solid-atmosphere coupling codes. These perturbations are a due to acoustic waves creating vertical velocities up to 130 m/s. Amplitudes and arrival times of these perturbations are reproduced respectively within a factor 2, and within a 60?s time window. Waveforms present a good agreement with observed data. The vertical acceleration to air density perturbation ratio is higher for these acoustic waves than for gravity waves. Combining these two pieces of information offers a new way to distinguish between these two wave types. This new type of data is a benchmark for the models of solid-atmosphere coupling. Amplitude and frequency content constrain the infrasound attenuation related to atmosphere viscosity and thermal conductivity. Observed time shifts between data and synthetics are ascribed to lateral variations of the seismic and atmospheric sound velocities and to the influence of atmospheric winds. These effects should be included in future modeling. This validation of our modeling tools allows to specify more precisely future observation projects.Space EngineeringAerospace Engineerin
One-Step Convergent Synthesis of the Steroid Ring System via the Coupling of γ,δ-Unsaturated Fischer Carbene Complexes with o
Total synthesis of (-)-CP<inf>2</inf>-disorazole C<inf>1</inf>
The total synthesis of a bis-cyclopropane analog of the antimitotic natural product (-)-disorazole C1 was accomplished in 23 steps and 1.1% overall yield. A vinyl cyclopropane cross-metathesis reaction generated a key (E)-alkene segment of the target molecule. IC50 determinations of (-)-CP2-disorazole C1 in human colon cancer cell lines indicated low nanomolar cytotoxic properties. Accordingly, this synthetic bioisostere represents the first biologically active disorazole analog not containing a conjugated diene or polyene substructure element. © 2011 American Chemical Society