Search results for: Giulia Loi

Items from 1 to 19 out of 19 results

article

HO‐1 downregulation favors BRAF^V600 melanoma cell death induced by Vemurafenib/PLX4032 and increases NK recognition

Anna L. Furfaro, Selene Ottonello, Giulia Loi, Irene Cossu, more

International Journal of Cancer > 146 > 7 > 1950 - 1962

Heme oxygenase 1 (HO‐1) plays a pivotal role in preventing cell damage. Indeed, through the antioxidant, antiapoptotic and anti‐inflammatory properties of its metabolic products, it favors cell adaptation against different stressors. However, HO‐1 induction has also been related to the gain of resistance to therapy in different types of cancers and its involvement in cancer immune‐escape has been...

article

Intraoperative parathyroid hormone (PTH) testing in patients with primary hyperparathyroidism and PTH levels in the normal range

Fabio Medas, Enrico Erdas, Giulia Loi, Francesco Podda, more

BMC Surgery > 2019 > 18 > 1 > 1-6

Background Primary hyperparathyroidism is a common endocrine disorder. Hypercalcemia with normal PTH levels is very unusual and can lead to diagnostic difficulties. There are very few very few studies in the literature and all with limited numerical samples. The goal of the present study was to determine the real incidence and characteristics of primary hyperparathyroidism with normal PTH and to evaluate...

article

Discovery of benzophosphadiazine drug candidate IDX375: A novel hepatitis C allosteric NS5B RdRp inhibitor

Jean-Laurent Paparin, Agnès Amador, Eric Badaroux, Stéphanie Bot, more

Bioorganic & Medicinal Chemistry Letters > 2017 > 27 > 11 > 2634-2640

Hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) plays a central role in virus replication. NS5B has no functional equivalent in mammalian cells, and as a consequence is an attractive target for selective inhibition. This paper describes the discovery of a novel family of HCV NS5B non-nucleoside inhibitors inspired by the bioisosterism between sulfonamide and phosphonamide. Systematic...

article

Parathyroidectomy for primary hyperparathyroidism in the elderly: experience of a single endocrine surgery center

Pietro Giorgio Calò, Fabio Medas, Giulia Loi, Giuseppe Pisano, more

Aging Clinical and Experimental Research > 2017 > 29 > 1 > 15-21

Background Primary hyperparathyroidism is a common endocrine disease, and its incidence increases with age. Aims Our aim was to retrospectively evaluate the impact of age on patient outcomes following parathyroidectomy for primary hyperparathyroidism. Methods Two-hundred fifty-six consecutive patients undergoing parathyroidectomy with preoperative diagnosis of primary hyperparathyroidism were...

article

Synthesis of potent and broad genotypically active NS5B HCV non-nucleoside inhibitors binding to the thumb domain allosteric site 2 of the viral polymerase

Claire Pierra Rouvière, Agnès Amador, Eric Badaroux, Thierry Convard, more

Bioorganic & Medicinal Chemistry Letters > 2016 > 26 > 18 > 4536-4541

The hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) plays a central role in virus replication. NS5B has no functional equivalent in mammalian cells and, as a consequence, is an attractive target for selective inhibition. This Letter describes the discovery of a new family of HCV NS5B non-nucleoside inhibitors, based on the bioisosterism between amide and phosphonamidate functions...

article

Controversies in the management of parathyroid carcinoma: A case series and review of the literature

Fabio Medas, Enrico Erdas, Giulia Loi, Francesco Podda, more

International Journal of Surgery > 2016 > 28 > S1 > S94-S98

Parathyroid carcinoma is a rare malignancy representing less than 1% of primary hyperparathyroidism cases. Its management is controversial due to lack of large-scale, multicentric studies. We report 8 new cases of parathyroid carcinoma and review the literature. Preoperative diagnosis of carcinoma was possible in 2 (25%) cases. Unclear surgical margins were present in 5 (62.5%) patients; 4 of them...

article

Feasibility of unilateral parathyroidectomy in patients with primary hyperparathyroidism and negative or discordant localization studies

Pietro Giorgio Calò, Fabio Medas, Giulia Loi, Enrico Erdas, more

Updates in Surgery > 2016 > 68 > 2 > 155-161

The purpose of this study was to examine the feasibility of unilateral parathyroidectomy in patients with primary hyperparathyroidism and negative or discordant localization studies. We included in our study 72 patients with preoperative diagnosis of primary hyperparathyroidism who had negative or discordant preoperative studies. In 66 patients, studies were discordant while in six were both negative...

article

Discovery and structural diversity of the hepatitis C virus NS3/4A serine protease inhibitor series leading to clinical candidate IDX320

Christophe C. Parsy, François-René Alexandre, Valérie Bidau, Florence Bonnaterre, more

Bioorganic & Medicinal Chemistry Letters > 2015 > 25 > 22 > 5427-5436

Exploration of the P2 region by mimicking the proline motif found in BILN2061 resulted in the discovery of two series of potent HCV NS3/4A protease inhibitors. X-ray crystal structure of the ligand in contact with the NS3/4A protein and modulation of the quinoline heterocyclic region by structure based design and modeling allowed for the optimization of enzyme potency and cellular activity. This research...

article

Synthesis and antiviral evaluation of a novel series of homoserine-based inhibitors of the hepatitis C virus NS3/4A serine protease

François-René Alexandre, Guillaume Brandt, Catherine Caillet, Dominique Chaves, more

Bioorganic & Medicinal Chemistry Letters > 2015 > 25 > 18 > 3984-3991

We disclose here the synthesis of a series of macrocyclic HCV protease inhibitors, where the homoserine linked together the quinoline P2′ motif and the macrocyclic moiety. These compounds exhibit potent inhibitory activity against HCV NS3/4A protease and replicon cell based assay. Their enzymatic and antiviral activities are modulated by substitutions on the quinoline P2′ at position 8 by methyl and...

article

Differentiated thyroid cancer in the elderly: Our experience

Pietro Giorgio Calò, Fabio Medas, Giulia Loi, Enrico Erdas, more

International Journal of Surgery > 2014 > 12 > S2 > S140-S143

Introduction: The objective of this retrospective study was to investigate clinical and pathologic characteristics of differentiated thyroid cancer in elderly patients and to evaluate the results of surgical treatment in this age group. Methods: The clinical records of patients who underwent total thyroidectomy between 2002 and 2012 with histopathological diagnosis of differentiated thyroid cancer...

article

Structure-based design of a novel series of azetidine inhibitors of the hepatitis C virus NS3/4A serine protease

Christophe Parsy, François-René Alexandre, Guillaume Brandt, Catherine Caillet, more

Bioorganic & Medicinal Chemistry Letters > 2014 > 24 > 18 > 4444-4449

Structural homology between thrombin inhibitors and the early tetrapeptide HCV protease inhibitor led to the bioisosteric replacement of the P2 proline by a 2,4-disubstituted azetidine within the macrocyclic β-strand mimic. Molecular modeling guided the design of the series. This approach was validated by the excellent activity and selectivity in biochemical and cell based assays of this novel series...

article

Novel Indolyl Aryl Sulfones Active against HIV-1 Carrying NNRTI Resistance Mutations: Synthesis and SAR Studies

Romano Silvestri, Gabriella De Martino, Giuseppe La Regina, Marino Artico, more

Journal of Medicinal Chemistry > 2003 > 46 > 12 > 2482 - 2493

article

Synthesis and studies of 3'-C-trifluoromethyl nucleoside analogues bearing adenine or cytosine as the base

Frédéric Jeannot, Gilles Gosselin, David Standring, Martin Bryant, more

Bioorganic & Medicinal Chemistry > 2002 > 10 > 10 > 3153-3161

3'-Deoxy-3'-C-CF ₃ , 2',3'-dideoxy-3'-C-CF ₃ and 2',3'-unsaturated-3'-C-CF ₃ nucleoside derivatives of adenosine and cytidine have been synthesized. All these derivatives were prepared by glycosylation of adenine and uracil with a suitable peracylated 3-trifluoromethyl sugar precursor. The resulting protected nucleosides were subject to appropriate chemical modifications to...

article

Synthesis, Biological Evaluation, and Binding Mode of Novel 1-[2-(Diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles Targeted at the HIV-1 Reverse Transcriptase

Romano Silvestri, Marino Artico, Gabriella De Martino, Rino Ragno, more

Journal of Medicinal Chemistry > 2002 > 45 > 8 > 1567 - 1576

article

Computer-assisted design, synthesis and biological evaluation of novel pyrrolyl heteroaryl sulfones targeted at HIV-1 reverse transcriptase as non-nucleoside inhibitors

Romano Silvestri, Marino Artico, Gabriella De Martino, Ettore Novellino, more

Bioorganic & Medicinal Chemistry > 2000 > 8 > 9 > 2305-2309

Three pyrrolyl heteroaryl sulfones (ethyl 1-[(1H-benzimidazol-2(3H)one-5-yl)sulfonyl]-1H-pyrrole-2-carboxylate, ethyl 1-[(1H-benzimidazol-5(6)-yl)sulfonyl]-1H-pyrrole-2-carboxylate and ethyl 1-[(1H-benzotriazol-5(6)-yl)sulfonyl]-1H-pyrrole-2-carboxylate) were designed as novel HIV-1 reverse transcriptase non-nucleoside inhibitors using structure-based computational methods. Although these compounds...

article

2-Triazenopyrroles: synthesis and biological activity

Patrizia Diana, Paola Barraja, Antonino Lauria, Anna Maria Almerico, more

European Journal of Medicinal Chemistry > 1999 > 34 > 4 > 353-360

2-Triazenopyrroles were synthesized by coupling the corresponding 2-diazopyrroles with secondary amines and tested for antiproliferative, antifungal, antiviral and antibacterial activities. Derivative 9m was the most cytotoxic, showing, against leukaemia, lymphoma and carcinoma cell lines, IC ₅ ₀ 3.9-21 μM and inhibited Cox-B2 and VSV with EC ₅ ₀ 10 μM. Derivative 9j, instead,...

article

Glycosidopyrroles Part 1. Acyclic derivatives: 1-(2-hydroxyethoxy) methylpyrroles as potential anti-viral agents

Anna Maria Almerico, Patrizia Diana, Paola Barraja, Gaetano Dattolo, more

Il Farmaco > 1998 > 53 > 1 > 33-40

Acyclic glycosidopyrroles of type 1, synthesized in good overall yields, were evaluated for anti-viral activity. Compound 10i was found to inhibit the HIV-1 replication at concentrations that were very close to those cytotoxic for MT-4 cells. Compounds 10a,f,i inhibited both strains HSV-1 and HSV-2 at concentrations slightly below those cytotoxic for Vero cells. However for this series of glycosidopyrroles...

article

1-arylsulfonyl-3-(α-hydroxybenzyl)-1H-pyrroles, a novel class of anti-HIV-1 reverse transcriptase inhibitors

Marino Artico, Roberto Di Santo, Roberta Costi, Silvio Massa, more

Bioorganic & Medicinal Chemistry Letters > 1997 > 7 > 14 > 1931-1936

Various 1-arylsulfonyl-3-(α-hydroxybenzyl)-1H-pyrroles were prepared by Friedel-Crafts reaction of 1-arylsulfonyl-1H-pyrroles with aroylchlorides in the presence of aluminum trichloride, followed by reduction of the ketones to the required carbinols. Title compounds were identified as a novel class of non-nucleoside HIV-1 reverse transcriptase inhibitors characterized by the presence of a diarylcarbinol...

article

5H-Pyrrolo[1,2-b][1,2,5]benzothiadiazepines (PBTDs): A Novel Class of Non-Nucleoside Reverse Transcriptase Inhibitors

Marino Artico, Romano Silvestri, Eugenia Pagnozzi, Giorgio Stefancich, more

Bioorganic & Medicinal Chemistry > 1996 > 4 > 6 > 837-850

With the aim of developing novel inhibitors of human immunodeficiency virus, various derivatives (10-17) related to 5H-pyrrolo[1,2-b][1,2,5]benzothiadiazepine (PBTD) were prepared and tested in vitro. The title tricyclic derivatives were obtained by intramolecular cyclization of the open-chain intermediate arylpyrrylsulfones, followed by N-alkylation at position 10. Among test derivatives some 10-alkyl-5H-pyrrolo[1,2-b][1,2,5]benzothiadiazepin-11(10H)-one-5,5-dioxides...

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