Context. The Gaia Data Release 1 (GDR1) is a first, important step on the path of evolution of astrometric accuracy towards a much improved situation. Although asteroids are not present in GDR1, this ...intermediate release already impacts asteroid astrometry. Aims. Our goal is to investigate how the GDR1 can change the approach to a few typical problems, including the determination of orbits from short-arc astrometry, the exploitation of stellar occultations, and the impact risk assessment. Methods. We employ optimised asteroid orbit determination tools, and study the resulting orbit accuracy and post-fit residuals. For this goal, we use selected ground-based asteroid astrometry, and occultation events observed in the past. All measurements are calibrated by using GDR1 stars. Results. We show that, by adopting GDR1, very short measurement arcs can already provide interesting orbital solutions, capable of correctly identifying near-Earth asteroids (NEAs) and providing a much more accurate risk rating. We also demonstrate that occultations, previously used to derive asteroid size and shapes, now reach a new level of accuracy at which they can be fruitfully used to obtain astrometry at the level of accuracy of Gaia star positions.
Abstract
We use data from five stellar occultations observed between 2013 and 2016 to constrain Chariklo’s size and shape, and the ring reflectivity. We consider four possible models for Chariklo ...(sphere, Maclaurin spheroid, triaxial ellipsoid, and Jacobi ellipsoid), and we use a Bayesian approach to estimate the corresponding parameters. The spherical model has a radius
R
= 129 ± 3 km. The Maclaurin model has equatorial and polar radii
and
, respectively, with density
. The ellipsoidal model has semiaxes
,
, and
. Finally, the Jacobi model has semiaxes
a
= 157 ± 4 km,
b
= 139 ± 4 km, and
c
= 86 ± 1 km, and density
. Depending on the model, we obtain topographic features of 6–11 km, typical of Saturn icy satellites with similar size and density. We constrain Chariklo’s geometric albedo between 3.1% (sphere) and 4.9% (ellipsoid), while the ring
I
/
F
reflectivity is less constrained between 0.6% (Jacobi) and 8.9% (sphere). The ellipsoid model explains both the optical light curve and the long-term photometry variation of the system, giving a plausible value for the geometric albedo of the ring particles of 10%–15%. The derived mass of Chariklo of 6–8 × 10
18
kg places the rings close to 3:1 resonance between the ring mean motion and Chariklo’s rotation period.
(+)-Narciclasine (2) available in quantity from certain Amaryllidaceae species or by total synthesis was employed as a precursor for a 10-step synthetic conversion (3.6% overall yield) to natural ...(+)-pancratistatin (1a). The key procedures involved epoxidation of natural (+)-narciclasine (2) to epoxide 6, reduction to diol 8, and formation of cyclic sulfate 12 and its ring opening with cesium benzoate followed by saponification of the benzoate to afford (+)-pancratistatin (1a).
A structure-activity relationship (SAR) study of the South African willow tree (Combretum caffrum) antineoplastic constituent combretastatin A-4 (1b) directed at maintaining the (Z)-stilbene ...relationship of the olefin diphenyl substituents led to synthesis of a potent cancer cell growth inhibitor designated phenstatin (3b). Initially phenstatin silyl ether (3a) was unexpectedly obtained by Jacobsen oxidation of combretastatin A-4 silyl ether (1c --> 3a), and the parent phenstatin (3b) was later synthesized (6a --> 3a --> 3b) in quantity. Phenstatin was converted to the sodium phosphate prodrug (3d) by a dibenzyl phosphite phosphorylation and subsequent hydrogenolysis sequence (3b --> 3c --> 3d). Phenstatin (3b) inhibited growth of the pathogenic bacterium Neisseriagonorrhoeae and was a potent inhibitor of tubulin polymerization and the binding of colchicine to tubulin comparable to combretastatin A-4 (1b). Interestingly, the prodrugs were found to have reduced activity in these biochemical assays. While no significant tubulin activity was observed with the phosphorylated derivative of combretastatin A-4 (1d), phosphate 3d retained detectable inhibitory effects in both assays.
Pluto and its main satellite, Charon, occulted the same star on 2008 June 22. This event was observed from Australia and La Reunion Island, providing the east and north Charon Plutocentric offset in ...the sky plane (J2000): X= + 12,070.5 ? 4 km (+ 546.2 ? 0.2 mas), Y= + 4,576.3 ? 24 km (+ 207.1 ? 1.1 mas) at 19:20:33.82 UT on Earth, corresponding to JD 2454640.129964 at Pluto. This yields Charon's true longitude L= 153.483 ? 0071 in the satellite orbital plane (counted from the ascending node on J2000 mean equator) and orbital radius r= 19,564 ? 14 km at that time. We compare this position to that predicted by (1) the orbital solution of Tholen & Buie (the 'TB97' solution), (2) the PLU017 Charon ephemeris, and (3) the solution of Tholen et al. (the 'T08' solution). We conclude that (1) our result rules out solution TB97, (2) our position agrees with PLU017, with differences of Delta *DL= + 0.073 ? 0071 in longitude, and Delta *Dr= + 0.6 ? 14 km in radius, and (3) while the difference with the T08 ephemeris amounts to only Delta *DL= 0.033 ? 0071 in longitude, it exhibits a significant radial discrepancy of Delta *Dr= 61.3 ? 14 km. We discuss this difference in terms of a possible image scale relative error of 3.35 X 10--3in the 2002-2003 Hubble Space Telescope images upon which the T08 solution is mostly based. Rescaling the T08 Charon semi-major axis, a = 19, 570.45 km, to the TB97 value, a = 19636 km, all other orbital elements remaining the same ('T08/TB97' solution), we reconcile our position with the re-scaled solution by better than 12 km (or 0.55 mas) for Charon's position in its orbital plane, thus making T08/TB97 our preferred solution.
A structure−activity relationship (SAR) study of the South African willow tree (Combretum caffrum) antineoplastic constituent combretastatin A-4 (3b) led to the discovery of a potent cancer cell ...growth inhibitor designated phenstatin (5a). This benzophenone derivative of combretastatin A-4 showed remarkable antineoplastic activity, and the benzophenone derivative of combretastatin A-1 was therefore synthesized. The benzophenone, designated hydroxyphenstatin (6a), was synthesized by coupling of a protected bromobenzene and a benzaldehyde to give the benzhydrol with subsequent oxidation to the ketone. Hydroxyphenstatin was converted to the sodium phosphate prodrug (6e) by a dibenzyl phosphite phosphorylation and subsequent benzyl cleavage (6a → 6d → 6e). While hydroxyphenstatin (6a) was a potent inhibitor of tubulin polymerization with activity comparable to that of combretastatin A-1 (3a), the phosphorylated derivative (6e) was inactive.
Continued investigation of cancer-cell growth-inhibitory constituents of the blue marine sponge Cribrochalina sp. has led to discovery of cribrostatins 3 (4a), 4 (5), and 5 (4b) in 10-5 to 10-7 % of ...the wet weight. The structure of cribrostatin 3 (4a) was determined by results of high field (500 MHz) 1H and 13C NMR and HRMS interpretations. The same general approach to the structures of cribrostatins 4 (5) and 5 (4b) was completed by X-ray crystal structure determinations. Cribrostatins 3, 4, and 5 provided significant cancer cell line inhibitory activities. Cribrostatins 1 and 2 and the newly isolated cribrostatins 3−5 displayed antibacterial and/or antifungal activities.
In an attempt to develop biologically active compounds from the inactive trans isomer (3a) of stilbene 1a, after asymmetric dihydroxylation to optically pure (R,R)-diol 8 the unexpected racemic ...diphenylacetaldehyde (9) was generated via a Pinacol rearrangement. Several derivatives of diphenylacetaldehyde 9 were synthesized (11-15) and reported. Further reaction of aldehyde 9 during desilylation through autoxidative decarbonylation afforded benzophenone 2b, designated hydroxyphenstatin, a potent antitumor and antimitotic agent. Hydroxyphenstatin showed potent inhibition of the tubulin assembly (IC(50) 0.82 microM) and exhibited an ED(50) of 2.5 microg/mL against the P388 lymphocytic leukemia cell line.
The South African willow tree Combretum caffrum has yielded a number of potent cancer cell growth inhibitors. The present SAR studies of the antineoplastic agent combretastatin A-4 (1c) were focused ...mainly on the olefinic bridge to determine the effects on cancer cell growth and, potentially, to better define the combretastatin A-4 binding site on tubulin. The geometric trans-isomer 3a of combretastatin A-4 was converted to the (1S,2S)- and (1R,2R)-vicinal diols 4c and 4d, respectively, under Sharpless' asymmetric dihydroxylation conditions. Cancer cell line testing showed the (1S,2S)-diol 4c to be more potent than its enantiomer 4d. Diol 4c weakly inhibited tubulin polymerization (IC50 = 22 μM, versus 1.2 μM for combretastatin A-4), while 4d was inactive (IC50 > 40 μM). Esterification of either stereoisomer at the diol and/or phenolic positions resulted in elimination of inhibitory activity.
Bioassay-guided isolation procedures using human tumor cell lines led to isolation of dibromophakellstatin (4) from the Republic of Seychelles sponge Phakellia mauritiana. The isolation, X-ray ...crystal structure elucidation, absolute stereochemistry, and antineoplastic activity have been summarized. P. mauritiana was also found to contain dibromophakellin (1), debromohymenialosine (2), thymidine, deoxyuridine, and thymine.
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