Search results for: Francesca Orlandi

Items from 1 to 8 out of 8 results

article

Safety assessment of a formulation for 68Ga-DOTATOC (68Ga-edotreotide or 68Ga-DOTA0-Tyr3-octreotide) preparation: Case studies in rats and rabbits

Daniela Chicco, Francesca Orlandi, Silvana Venturella, Paola Di Manno, more

Journal of Pharmacological and Toxicological Methods > 2016 > 81 > C > 379-380

article

Substituted piperazines as nootropic agents: 2- or 3-phenyl derivatives structurally related to the cognition-enhancer DM235

Luca Guandalini, Maria Vittoria Martino, Lorenzo Di Cesare Mannelli, Gianluca Bartolucci, more

Bioorganic & Medicinal Chemistry Letters > 2015 > 25 > 8 > 1700-1704

A series of 2-phenyl- or 3-phenyl piperazines, structurally related to DM235 and DM232, two potent nootropic agents, have been prepared and tested in the mouse passive-avoidance test, to assess their ability to revert scopolamine-induced amnesia. Although the newly synthesized molecules were less potent than the parent compounds, some useful information has been obtained from structure–activity relationships...

article

New structure–activity relationship studies in a series of N,N-bis(cyclohexanol)amine aryl esters as potent reversers of P-glycoprotein-mediated multidrug resistance (MDR)

Francesca Orlandi, Marcella Coronnello, Cristina Bellucci, Silvia Dei, more

Bioorganic & Medicinal Chemistry > 2013 > 21 > 2 > 456-465

As a continuation of previous research on a new series of potent and efficacious P-gp-dependent multidrug resistant (MDR) reversers with a N,N-bis(cyclohexanol)amine scaffold, we have designed and synthesized several analogs by modulation of the two aromatic moieties linked through ester functions to the N,N-bis(cyclohexanol)amine, aiming to optimize activity and to extend structure–activity relationships...

article

Combination of epitope-optimized DNA vaccination and passive infusion of monoclonal antibody against HER2/neu leads to breast tumor regression in mice

Francesca Orlandi, José A. Guevara-Patiño, Taha Merghoub, Jedd D. Wolchok, more

Vaccine > 2011 > 29 > 20 > 3646-3654

HER2/neu is an oncogene amplified and over-expressed in 20-30% of breast adenocarcinomas. Treatment with the humanized monoclonal antibody trastuzumab has shown efficacy in combination with cytotoxic agents, although resistance occurs over time. Novel approaches are needed to further increase antibody efficacy. In this study, we provide evidence in a mouse breast cancer therapeutic tumor model that...

article

Inhibition of P-glycoprotein-mediated Multidrug Resistance (MDR) by N,N-bis(cyclohexanol)amine aryl esters: Further restriction of molecular flexibility maintains high potency and efficacy

Cecilia Martelli, Silvia Dei, Catherine Lambert, Dina Manetti, more

Bioorganic & Medicinal Chemistry Letters > 2011 > 21 > 1 > 106-109

Conformational modulation of the aryl portion of a set of N,N-bis(cyclohexanol)amine aryl esters (1a–d) that are potent Pgp-dependent MDR inhibitors has been performed. Toward this end the trans-3-(3,4,5-trimethoxyphenyl)acrylic acid present in set 1 was substituted with 3-(3,4,5-trimethoxyphenyl)propanoic and 3-(3,4,5-trimethoxyphenyl)propiolic moieties to give sets 2 and 3, respectively. While the...

article

Structure−Activity Relationships Studies in a Series of N , N -Bis(alkanol)amine Aryl Esters as P-Glycoprotein (Pgp) Dependent Multidrug Resistance (MDR) Inhibitors ^†

Cecilia Martelli, Marcella Coronnello, Silvia Dei, Dina Manetti, more

Journal of Medicinal Chemistry > 2010 > 53 > 4 > 1755 - 1762

article

Synthesis, Affinity Profile and Functional Activity of Potent Chiral Muscarinic Antagonists with a Pyrrolidinylfuran Structure ^†

Serena Scapecchi, Marta Nesi, Rosanna Matucci, Cristina Bellucci, more

Journal of Medicinal Chemistry > 2010 > 53 > 1 > 201 - 207

article

Immunological validation of the EpitOptimizer program for streamlined design of heteroclitic epitopes

Colin S.B. Houghton, Manuel E. Engelhorn, Cailan Liu, Da Song, more

Vaccine > 2007 > 25 > 29 > 5330-5342

One strategy to generate T-cell responses to tumors is to alter subdominant epitopes through substitution of amino acids that are optimal anchors for specific MHC molecules, termed heteroclitic epitopes. This approach is manually error-prone and time-consuming. In here, we describe a computer-based algorithm (EpitOptimizer) for the streamlined design of heteroclitic epitopes. Analysis of two cancer-related...

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CHEMOSENSITIZERS (2)
DOXORUBICIN-RESISTANT ERYTHROLEUKEMIA K562 CELLS (K562/DOX) (2)
N,N-BIS(CYCLOHEXANOL)AMINE ARYL ESTERS (2)
PIRARUBICIN UPTAKE (2)
ANTIGENS/PEPTIDES/EPITOPES (1)
BREAST CANCER (1)
COGNITION-ENHANCERS (1)
DNA VACCINE (1)
HER2/NEU (1)
IMMUNOTHERAPY (1)
MDR REVERSERS (1)
MDR REVERTERS (1)
MOUSE PASSIVE-AVOIDANCE TEST (1)
P-GP INHIBITORS (1)
PGP INHIBITORS (1)
PIPERAZINES (1)
PIRACETAM-LIKE COMPOUNDS (1)
SUNIFIRAM (1)
T CELLS (1)
TUMOR IMMUNITY (1)
VACCINATION (1)
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Elsevier (6)
ACS (2)

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Search results for: Francesca Orlandi

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