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1.
Sensors (Basel) ; 12(3): 2954-68, 2012.
Article in English | MEDLINE | ID: mdl-22736986

ABSTRACT

An electronic meter to measure surface seawater density is presented. It is based on the measurement of the difference in displacements of a surface level probe and a weighted float, which according to Archimedes' law depends on the density of the water. The displacements are simultaneously measured using a high-accuracy magnetostrictive sensor, to which a custom electronic board provides a wireless connection and power supply so that it can become part of a wireless sensor network. The electronics are designed so that different kinds of wireless networks can be used, by simply changing the wireless module and the relevant firmware of the microcontroller. Lastly, laboratory and at-sea tests are presented and discussed in order to highlight the functionality and the performance of a prototype of the wireless density meter node in a Bluetooth radio network. The experimental results show a good agreement of the values of the calculated density compared to reference hydrometer readings.


Subject(s)
Seawater/analysis , Wireless Technology , Algorithms , Electronics , Wireless Technology/instrumentation
2.
J Med Chem ; 52(23): 7512-27, 2009 Dec 10.
Article in English | MEDLINE | ID: mdl-19601594

ABSTRACT

New arylthioindoles along with the corresponding ketone and methylene compounds were potent tubulin assembly inhibitors. As growth inhibitors of MCF-7 cells, sulfur derivatives were superior or sometimes equivalent to the ketones, while methylene derivatives were substantially less effective. Esters 24, 27-29, 36, 39, and 41 showed approximately 50% of inhibition on human HeLa and HCT116/chr3 cells at 0.5 microM, and these compounds inhibited the growth of HEK, M14, and U937 cells with IC(50)'s in the 78-220 nM range. While murine macrophage J744.1 cell growth was significantly less affected (20% at higher concentrations), four other nontransformed cell lines remained sensitive to these esters. The effect of drug treatment on cell morphology was examined by time-lapse microscopy. In a protocol set up to evaluate toxicity on the Saccharomyces cerevisiae BY4741 wild type strain, compounds 24 and 54 strongly reduced cell growth, and 29, 36, and 39 also showed significant inhibition.


Subject(s)
Indoles/chemistry , Indoles/pharmacology , Models, Molecular , Protein Multimerization/drug effects , Sulfur/chemistry , Tubulin/metabolism , Cell Line, Tumor , Cell Proliferation/drug effects , Colchicine/metabolism , Humans , Indoles/chemical synthesis , Indoles/metabolism , Inhibitory Concentration 50 , Protein Structure, Quaternary , Structure-Activity Relationship , Tubulin/chemistry
3.
Bioorg Med Chem ; 16(18): 8419-26, 2008 Sep 15.
Article in English | MEDLINE | ID: mdl-18755591

ABSTRACT

Molecules that target microtubules have an important role in the treatment of cancer. A new class of inhibitors of tubulin polymerization based on the 2-(3,4,5-trimethoxybenzoyl)-2-dimethylamino-benzo[b]furan molecular skeleton was synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization, and cell cycle effects. The most promising compound in this series was 2-(3,4,5-trimethoxybenzoyl)-3-dimethylamino-6-methoxy-benzo[b]furan, which inhibits cancer cell growth at nanomolar concentrations and interacts strongly with tubulin by binding to the colchicine site.


Subject(s)
Antimitotic Agents/pharmacology , Benzofurans/pharmacology , Cell Proliferation/drug effects , Tubulin Modulators/pharmacology , Animals , Antimitotic Agents/chemical synthesis , Benzofurans/chemical synthesis , Cell Line, Tumor , Humans , Inhibitory Concentration 50 , Mice , Protein Binding , Structure-Activity Relationship , Tubulin Modulators/chemical synthesis , Tumor Cells, Cultured
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