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Your search keyword '"FUNICELLO, M."' showing total 104 results
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104 results on '"FUNICELLO, M."'

4. Two novel precursors of the hiv-1 protease inhibitor darunavir target the upr/proteasome system in human hepatocellular carcinoma cell line hepg2

Author

Rinaldi, R., Miglionico, R., Nigro, I., D'Orsi, R., Chiummiento, L., Funicello, M., Lupattelli, P., Laurenzana, I., Sgambato, Alessandro, Monne, M., Bisaccia, F., Armentano, M. F., Sgambato A. (ORCID:0000-0002-9487-4563), Rinaldi, R., Miglionico, R., Nigro, I., D'Orsi, R., Chiummiento, L., Funicello, M., Lupattelli, P., Laurenzana, I., Sgambato, Alessandro, Monne, M., Bisaccia, F., Armentano, M. F., and Sgambato A. (ORCID:0000-0002-9487-4563)

Abstract

Background: Several pre-clinical and clinical reports suggest that HIV-1 protease inhibitors, in addition to the antiretroviral properties, possess pleiotropic pharmacological effects including anti-cancer action. Therefore, we investigated the pro-apoptotic activity in tumor cells of two molecules, RDD-19 and RDD-142, which are hydroxyethylamine derivatives’ precursors of darunavir and several HIV-1 protease inhibitors. Methods: Three hepatoma cell lines and one non-pathological cell line were treated with RDD-19 and RDD-142, and cell viability was assessed. The expression levels of several markers for ER stress, autophagy, cellular ubiquitination, and Akt activation were quantified in HepG2 cells treated with RDD-19 and RDD-142 to evaluate apoptotic and non-apoptotic cell death. Results: RDD-19 and RDD-142 showed a greater dose-dependent cytotoxicity towards the hepatic tumor cell line HepG2 compared to the non-pathological hepatic cell line IHH. Both molecules caused two types of cell death, a caspase-dependent apoptosis, which was ascertained by a series of biochemical and morphological assays, and a caspase-independent death that was characterized by the induction of ER stress and autophagy. The strong increase of ubiquitinated proteins inside the cells suggested that the target of these molecules could be the proteasome and in silico molecular docking analysis that was used to support the plausibility of this hypothesis. Furthermore, cells treated with the two compounds displayed decreased levels of p-AKT, which interferes with cell survival and proliferation. Conclusions: These findings demonstrate that two compounds, RDD-19 and RDD-142, have pleiotropic effects and that they may represent promising anticancer candidates.

Published
2021

5. Regio- and Diastereoselective Organo-Zinc-Promoted Arylation of trans-2,3-Diaryloxiranes by Arylboronic Acids: Stereoselective Access to trans-2,3-Diphenyl-2,3-dihydrobenzofuran

Author

Laurita T., Chiummiento L., Funicello M., D'Orsi R., Sallemi D., Tofani D., Lupattelli P., Laurita, T., Chiummiento, L., Funicello, M., D'Orsi, R., Sallemi, D., Tofani, D., and Lupattelli, P.

Subjects
2,3-Dihydrobenzofuran, Ring opening reaction, Diaryloxirane, Arylzinc reagent
Abstract

ortho-Oxo substituted trans 2,3-diaryloxiranes were regio- and stereoselectively arylated by arylzinc reagents, obtained from the corresponding boronic acids by B–Zn exchange. The reaction was quite general, irrespective to the aryl nucleophile and proceeded via a ring opening at the α-carbon with respect to the substituted aryl ring. The stereoselectivity was from high to complete toward the alcohol resulted from retention of configuration at the electrophilic carbon. The method allowed a direct and high yielding access to trans 2,3-diphenyl-2,3-dihydrobenzofuran, which is a key structural motif in resveratrol dimers as viniferins. The use of enantioenriched starting diaryloxiranes resulted in no loss of stereochemical integrity in the final trans 2,3-dihydrobenzofuran, which was characterized for the first time in enantioenriched form.

Published
2019

41. Organometallics in Water:  Three-Coordinate [Pt<SUP>0</SUP>(N,N-chelate)(η<SUP>2</SUP>-olefin)] Complexes Containing New Chiral Ligands Based on α-<SCP>d</SCP>-Mannose

Author

Ferrara, M. L., Orabona, I., Ruffo, F., Funicello, M., and Panunzi, A.

Abstract

New bidentate nitrogen ligands based on α-D-mannose were prepared and investigated by preparing a family of platinum(0) complexes of formula [Pt(N,N-chelate)(η2-olefin)]. The ability of one N,N-chelate to induce a stereoselective reaction in water was assessed.

Published
1998

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