Publications

A Convenient Route to 3′‐Deoxy‐α‐ L ‐ and 3′‐Deoxy‐β‐ D ‐apionucleosides The cyclic thionocarbonate 3 , easily available in three steps from 3′‐ O ‐benzoyl‐2,3‐ O ‐isopropylidene‐ D ‐apio‐β‐ D ‐furanose ( 1 ), is deoxygenated with n ‐Bu 3 SnH to yield the 3′‐deoxy epimers 4 [methyl 3‐C‐(benzoyloxymethyl)‐3‐deoxy‐α‐ L ‐ threo ‐tetrofuranoside] and 6 [methyl 3‐ C ‐(benzoyloxymethyl)‐3‐deoxy‐β‐ D ‐ erythro ‐tetrofuranoside]. These are separated by chromatography and further converted to the 3′‐deoxy‐α‐ L ‐apionucleosides 11–13 , and the 3′‐deoxy‐β‐ D ‐apionucleosides 17–19 , respectively.

We here report that after infection with human herpesvirus 6A, human cord blood mononuclear cells accumulate in G 2 /M phase of the cell cycle. Experiments with foscarnet or ultraviolet (UV)‐irradiated virus stocks pointed at an (immediate‐)early, newly formed viral protein to be responsible for the arrest. At the molecular level, p53, cyclin B 1 , cyclin A and tyrosine 15 ‐phosphorylated cdk1 accumulated after HHV‐6A infection, indicating an arrest in G 2 . However, no change was observed in the levels of downstream effectors of p53 in establishing a G 2 arrest, i.e. p21 and 14‐3‐3σ. We thus conclude that the HHV‐6A‐induced G 2 arrest occurs independently of p53 accumulation.

No abstract is provided for this article.

Cracks and delamination, resulting from residual stresses, are a barrier in the world of additive manufacturing and selective laser melting (SLM) that prohibits the use of many metals in this field. By preheating the baseplate, thermal gradients are lowered and stresses can be reduced. In this work, some initial tests were performed with M2 high speed steel (HSS). The influence of preheating on density and mechanical and physical properties is investigated. The paper shows many promising results for the production of SLM parts in materials that are very sensitive to crack formation and delamination. When using a preheating of 200 °C, crack-free M2 HSS parts were produced with a relative density of 99.8%.

A series of 38 2-naphthyl-substituted diarylpyrimidine (DAPY) analogues, characterized by various substitution patterns on the pyrimidine and naphthalene rings, was synthesized in a straightforward fashion by means of parallel synthesis and evaluated as inhibitors of the HIV-1 wild-type and double mutant (K103N+Y181C) strains. Most of the compounds displayed strong activity against wild-type HIV-1. The most active compound, with a cyano group at position C6 on the naphthalene ring, exhibited activity against wild-type HIV-1 with an EC50 value of 0.002 microM and against the double mutant strain with an EC50 value of 0.24 microM; the selectivity index (SI) against wild-type is >180 000, the highest SI value among DAPY analogues. The structure-activity relationship (SAR) of the newly synthesized DAPYs is presented herein.

In December 1995, a 70-years old male was referred to us because of rapid visual loss in the right eye, one month after a central retinal artery occlusion in the left eye. This renal transplant patient, with limited renal function, was on immunosuppressive therapy. The diagnosis of bilateral progressive outer retinal necrosis (PORN) due to varicella-zoster virus (VZV) was confirmed by polymerase chain reaction (PCR) detection of VZV DNA in the aqueous fluid. As retinitis progressed despite of intravenous acyclovir administration, the antiviral therapy was switched to oral bromovinyldeoxyuridine (BVDU). This case-report demonstrates that oral BVDU can be a good alternative to acyclovir for the treatment of VZV retinal infections.

Abstract The addition reaction of either 3-bromo-5-lithiopyridine (2a) or 3-cyano-5-lithiopyridine (2b) to 2,4:3,5-di-O-benzylidene-aldehydo-D-xylose (1) gave a D-gulo/D-ido mixture of respectively 3-bromo- and 3-cyano-5-(2,4;3,5-di-O-benzylidene-pentitol-1-yl)pyridine (3a, b). Mesylation of C-1′ followed by reaction with CF3COOH/H2O resulted in the formation of the corresponding D-xylo-furanosyl pyridine C-nucleosides. 3-Cyano-5-D-xylofuranosylpyridine (5b) was converted to 3-carbamoyl-5-D-xylofuranosylpyridine (6) with Amberlite IRA 400 (OH−). The D-xylofuranosyl C-nucleosides were evaluated for their antiviral and cytostatic activity. No significant activity was found.