| 1. |
- Almqvist, Fredrik, et al.
(författare)
-
Spirobicyclo[2.2.2]octane derivatives: mimetics of baccatin III and paclitaxel (Taxol)
- 2004
-
Ingår i: Organic and Biomolecular Chemistry. - 1477-0539. ; 2:21, s. 3085-3090
-
Tidskriftsartikel (refereegranskat)abstract
- The formylated spirobyclic alcohol 8a was computer modeled to be a mimetic of paclitaxel. In this model, the formyl group was used as a truncated paclitaxel side chain in order to reduce the computational work. Compound 8c, carrying the paclitaxel side chain, was synthesized in six steps from optically active 1,3-diketone 12. Microtubule stabilization was not observed for 8c, indicating that the model needs to be adjusted.
|
|
| 2. |
- Almqvist, Fredrik, et al.
(författare)
-
Spirobicyclo[2.2.2]octane derivatives: mimetics of baccatin III and paclitaxel (Taxol)
- 2004
-
Ingår i: ORGANIC & BIOMOLECULAR CHEMISTRY. - : Royal Society of Chemistry (RSC). - 1477-0520 .- 1477-0539. ; 2:21, s. 3085-90
-
Tidskriftsartikel (refereegranskat)abstract
- The formylated spirobyclic alcohol 8a was computer modeled to be a mimetic of paclitaxel. In this model, the formyl group was used as a truncated paclitaxel side chain in order to reduce the computational work. Compound 8c, carrying the paclitaxel side chain, was synthesized in six steps from optically active 1,3-diketone 12. Microtubule stabilization was not observed for 8c, indicating that the model needs to be adjusted.
|
|
| 3. |
|
|
| 4. |
- Bache, Iben, et al.
(författare)
-
An excess of chromosome 1 breakpoints in male infertility.
- 2004
-
Ingår i: European Journal of Human Genetics. - : Springer Science and Business Media LLC. - 1476-5438 .- 1018-4813. ; 12:12, s. 993-1000
-
Tidskriftsartikel (refereegranskat)abstract
- In a search for potential infertility loci, which might be revealed by clustering of chromosomal breakpoints, we compiled 464 infertile males with a balanced rearrangement from Mendelian Cytogenetics Network database (MCNdb) and compared their karyotypes with those of a Danish nation-wide cohort. We excluded Robertsonian translocations, rearrangements involving sex chromosomes and common variants. We identified 10 autosomal bands, five of which were on chromosome 1, with a large excess of breakpoints in the infertility group. Some of these could potentially harbour a male-specific infertility locus. However, a general excess of breakpoints almost everywhere on chromosome 1 was observed among the infertile males: 26.5 versus 14.5% in the cohort. This excess was observed both for translocation and inversion carriers, especially pericentric inversions, both for published and unpublished cases, and was significantly associated with azoospermia. The largest number of breakpoints was reported in 1q21; FISH mapping of four of these breakpoints revealed that they did not involve the same region at the molecular level. We suggest that chromosome 1 harbours a critical domain whose integrity is essential for male fertility.
|
|
| 5. |
- Belda, Oscar, et al.
(författare)
-
Chiral bispyridylamide metal complexes as catalysts for the enantioselective adddition of TMSCN to aldehydes
- 2004
-
Ingår i: Journal of Organometallic Chemistry. - : Elsevier BV. - 0022-328X .- 1872-8561. ; 689:23, s. 3750-3755
-
Tidskriftsartikel (refereegranskat)abstract
- The use of (1R,2R)-N,N'-bis(2-pyridinecarboxyamido)-1,2-diphenylethane metal complexes as catalysts for the enantioselective addition of trimethylsilyl cyanide to aldehydes is described. Enantioselectivities up to 70% ee were obtained with a Ti(IV) catalyst. Complexes with Zr(IV), Sc(III), Yb(III) and Cu(II) afforded less selective catalysts. For the Zr(IV) complex, a rate and selectivity enhancement was observed when adding 0.5 equiv. of water with respect to the catalyst. Studies of the metal complexes involved in the reaction were carried out by means of H-1 NMR spectroscopy. A Zr complex was shown by X-ray crystallography to exhibit distorted octahedral coordination, with the four nitrogen atoms of the doubly deprotonated ligand essentially in one plane.
|
|
| 6. |
- Bensing, Sophie, et al.
(författare)
-
No evidence for autoimmunity as a major cause of the empty sella syndrome
- 2004
-
Ingår i: Experimental and clinical endocrinology & diabetes. - : Georg Thieme Verlag KG. - 0947-7349 .- 1439-3646. ; 112:5, s. 231-235
-
Tidskriftsartikel (övrigt vetenskapligt/konstnärligt)abstract
- OBJECTIVE: The cause of empty sella syndrome (ESS) remains largely unknown. We measured eleven organ-specific autoantibodies in serum in order to evaluate possible autoimmune components in ESS. PATIENTS: Thirty patients with ESS and 50 healthy blood donors participated in the study. MEASUREMENTS: Detection of pituitary autoantibodies was performed by immunoblotting with human pituitary cytosol as antigen. Thyroid peroxidase (TPO) and TSH receptor (TRAK) autoantibodies were analysed by radioimmunoassay. The remaining eight autoantibodies were detected by in vitro transcription and translation of the autoantigens and immunoprecipitation. RESULTS: The majority of the ESS patients (18/30) exhibited no immunoreactivity at all. None of the remaining 12 ESS patients reacted against more than one autoantigen. No immunoreactivity was found more frequently among ESS patients than healthy blood donors. Pituitary autoantibodies were not correlated to the ESS patients' pituitary function or sellar size, although the results indicated a tendency of increased autoimmunity in patients with hypopituitarism and normal sella size respectively. CONCLUSION: Detection of autoantibodies is a valuable tool in the diagnostic work-up of autoimmune diseases. By analysing a large number of organ-specific autoantibodies we found no evidence of ESS being associated with any specific autoimmune disease. The pathogenesis of ESS is believed to be heterogeneous and our findings suggest autoimmune components to be of minor importance. In some selective cases, ESS in combination with hypopituitarism may be the result of an autoimmune disease in the pituitary gland but this needs further investigation.
|
|
| 7. |
|
|
| 8. |
|
|
| 9. |
- Bertilsson, Sophie
(författare)
-
Asymmetric Formation and Isomerization of Three-Membered Rings : Catalyst Development and Evaluation
- 2001
-
Doktorsavhandling (övrigt vetenskapligt/konstnärligt)abstract
- Enantiopure α-amino acid derivatives were prepared using a protocol which allows for highly controlled regio- and chemoselectivity in the hydrogenation/ hydrogenolysis of aza-Diels-Alder adducts. One of the resulting α-amino esters, (1S,3R,4R)-2-azabicyclo[2.2.1]heptane-3-carboxylic acid ethyl ester, was utilized further as a catalyst precursor. Significant improvements were achieved in the asymmetric lithium amide-mediated epoxide rearrangement reaction. An efficient catalytic system was developed, based on 5 mol% of (1S,3R,4R)-3-(amino)methyl-2-azabicyclo[2.2.1]heptanes and stoichiometric amounts of lithium diisopropylamide (LDA). With pyrrolidine or (2R,5R)-dimethylpyrrolidine as the amine moiety, the isomerization into allylic alcohols was accomplished for 5–7-membered cycloalkene oxides and (Z)-octene oxide with yields of >90% and enantioselectivities up to 99% ee. The studies indicate that the active catalyst species is a monomer, which is in equilibrium with inactive aggregates. The addition of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) led to a reaction rate acceleration. In the catalytic reaction, where there is a competing LDA-mediated rearrangement, the presence of DBU also improved the enantioselectivity. Furthermore, the asymmetric addition of carbenes and nitrenes to olefins was investigated. N,N'- and N,O-oxazolines were evaluated as ligands in the Cu-catalyzed aziridination of alkenes. Two of the oxazolines formed highly active catalysts (90% yield). However, the enantioselectivity was moderate (≤34% ee). Another catalyst, tetrakis-[(1S,3R,4R)-2-(p-tert-butylbenzene)sulphonyl-2-azabicyclo[2.2.1]heptane-3-carboxylate]dirhodium(II) was prepared and successfully applied in the reaction of styrenes and cyclic enol ethers with phenyl- and vinyldiazoacetates, affording cyclopropanes in up to 95% yield and 92% ee. In contrast to earlier observations, the best results were obtained with electron-rich olefins.
|
|
| 10. |
|
|
