Angelina Boccarelli

Inhibition of endothelial cell functions and of angiogenesis by the metastasis inhibitor NAMI-A

NAMI-A is a ruthenium-based compound with selective anti-metastasis activity in experimental models of solid tumours. We studied whether this activity was dependent on anti-angiogenic ability of NAMI-A. We thus investigated its in vitro effects on endothelial cell functions necessary for angiogenesis to develop, as well as its in vivo effects in the chick embryo chorioallantoic membrane model. Endothelial cell proliferation, chemotaxis, and secretion of the matrix-degrading enzyme metalloproteinase-2 were inhibited by NAMI-A in a dose-dependent manner, and without morphologic signs of cell apoptosis or necrosis. Lastly, NAMI-A displayed a dose-dependent in vivo anti-angiogenic activity in the chorioallantoic membrane model. These data suggest that the anti-angiogenic activity of NAMI-A can contribute to its anti-metastatic efficacy in mice bearing malignant solid tumours.

Platinum complexes with imino ethers or cyclic ligands mimicking imino ethers: synthesis, in vitro antitumour activity, and DNA interaction properties

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Breast Cancer’s Microarray Data: Pattern Discovery Using Nonnegative Matrix Factorizations

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A New Class of 1‐Aryl‐5,6‐dihydropyrrolo[2,1‐a]isoquinoline Derivatives as Reversers of P‐Glycoprotein‐Mediated Multidrug Resistance in Tumor Cells

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Effect of cisplatin containing liposomes formulated by unsaturated chain-containing lipids on gynecological tumor cells

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Platinum complexes can inhibit matrix metalloproteinase activity: platinum-diethyl[(methylsulfinyl)methyl]phosphonate complexes as inhibitors of matrix metalloproteinases 2, 3, 9, and 12.

(compounds 1–4 for trans geometry and 5–8 for cis geometry, respectively). The cyclic ligands mimic the imino ether ligands but, differently from imino ethers, cannot undergo change of configuration. In a panel of human tumor cells, trans compounds inhibit growth much more than transplatin. Moreover, compound 1 in most cases is less active than 2, and 1 and 2 are less active than 3 and 4, respectively. For cis compounds with imino ethers, the activity is reduced (5) or unaffected (6) with respect to cisplatin. Moreover, unlike trans compounds, substitution of cyclic ligands (7, 8) for imino ethers (5, 6) generally decreases the activity. This determines, for compounds with cyclic ligands, an unusual inversion of the cis geometry requirement for activity of platinum(II) species. Importantly, 1–4 and 5–8 partially circumvent the multifocal cisplatin resistance of A2780cisR cells, and 1–4 also overcome resistance from reduced uptake of 41McisR cells. DNA interaction regioselectivity of 1–4 and 5–8 is not substantially modified with respect to transplatin and cisplatin. However, both imino ethers and cyclic ligands slow down the DNA interstrand cross-link reaction, (E)-HN=C(OMe)Me and % MathType!Translator!2!1!AMS LaTeX.tdl!TeX -- AMS-LaTeX! <![CDATA[% MathType!MTEF!2!1!+- % feaafeart1ev1aaatCvAUfeBSn0BKvguHDwzZbqefeKCPfgBGuLBPn % 2BKvginnfarmWu51MyVXgatuuDJXwAK1uy0HwmaeHbfv3ySLgzG0uy % 0Hgip5wzaebbnrfifHhDYfgasaacH8YjY-vipgYlH8Gipec8Eeeu0x % Xdbba9frFj0-OqFfea0dXdd9vqai-hGuQ8kuc9pgc9q8qqaq-dir-f % 0-yqaiVgFr0xfr-xfr-xb9adbaqaaeGaciGaaiaabeqaamaabmabaa % GcbaWaaKraaeaacaqGobGaeyypa0Jaae4qaiaabIcacaqGnbGaaeyz % aiaabMcacaqGpbGaae4qaiaabIeadaWgaaWcbaGaaeOmaaqabaGcca % qGdbaaleaaaOGaayzdSdGaaeisamaaBaaaleaacaqGYaaabeaaaaa!45C8!