| 1. |
- Auzzas, Luciana, et al.
(författare)
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Non-natural macrocyclic inhibitors of histone deacetylases : design, synthesis, and activity
- 2010
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Ingår i: Journal of Medicinal Chemistry. - : American Chemical Society. - 0022-2623 .- 1520-4804. ; 53:23, s. 8387-8399
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Tidskriftsartikel (refereegranskat)abstract
- Nonpeptidic chiral macrocycles were designed on the basis of an analogue of suberoylanilide hydroxamic acid (2) (SAHA, vorinostat) and evaluated against 11 histone deacetylase (HDAC) isoforms. The identification of critical amino acid residues highly conserved in the cap region of HDACs guided the design of the suberoyl-based macrocycles, which were expected to bear a maximum common substructure required to target the whole HDAC panel. A nanomolar HDAC inhibitory profile was observed for several compounds, which was comparable, if not superior, to that of 2. A promising cytotoxic activity was found for selected macrocycles against lung and colon cancer cell lines. Further elaboration of selected candidates led to compounds with an improved selectivity against HDAC6 over the other isozymes. Pair-fitting analysis was used to compare one of the best candidates with the natural tetrapeptide apicidin, in an effort to define a general pharmacophore that might be useful in the design of surrogates of peptidic macrocycles as potent and isoform-selective inhibitors.
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| 2. |
- Meacci, Valentino, et al.
(författare)
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Real-time in-line industrial fluids characterization using multiple pulse repetition frequency
- 2019
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Ingår i: Part of the Lecture Notes in Electrical Engineering book series (LNEE, volume 512). - Cham : Springer International Publishing. - 9783319930817 ; , s. 73-79
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Konferensbidrag (refereegranskat)abstract
- The characterization of fluids flowing in industrial pipes is of paramount importance to optimize the production process and guarantee the final product quality in most industries. Rheological parameters of the fluid can be efficiently calculated starting from the Pressure Drop (PD) along a tract of the pipe, and the velocity profile that the flow develops along the pipe diameter, which can be assessed through Ultrasounds Pulsed Wave Doppler (PWD). Unfortunately, in PWD the maximum detectable velocity is restricted by the aliasing limit related to the Pulse Repetition Frequency (PRF). The use of PRF sequences at different rate can recover de-aliased velocities by combining the aliased data. In this work, we extend the capabilities of an embedded PWD ultrasound system used to characterize industrial fluids by implementing, in real-time, the multi-PRF method.
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