Search

Your search keyword '"Turlizzi E"' showing total 2 results
Start Over Author "Turlizzi E" Topic antineoplastic agents
2 results on '"Turlizzi E"'

1. Structure-activity relationship and properties optimization of a series of quinazoline-2,4-diones as inhibitors of the canonical Wnt pathway.

Author

Nencini A, Pratelli C, Quinn JM, Salerno M, Tunici P, De Robertis A, Valensin S, Mennillo F, Rossi M, Bakker A, Benicchi T, Cappelli F, Turlizzi E, Nibbio M, Caradonna NP, Zanelli U, Andreini M, Magnani M, and Varrone M

Subjects
Animals, Antineoplastic Agents metabolism, Antineoplastic Agents pharmacokinetics, Cell Line, Tumor, Cell Proliferation drug effects, Female, Humans, Inhibitory Concentration 50, Male, Mice, Quinazolines metabolism, Quinazolines pharmacokinetics, Structure-Activity Relationship, Xenograft Model Antitumor Assays, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Quinazolines chemistry, Quinazolines pharmacology, Wnt Signaling Pathway drug effects
Abstract

Wnt signaling pathway plays a critical role in numerous cellular processes, including tumor initiation, proliferation, invasion/infiltration, metastasis formation and resistance to chemotherapy. In a drug discovery project aimed at the identification of inhibitors of the canonical Wnt pathway, we selected a series of quinazoline 2,4-diones as starting point for the therapeutic treatment of glioblastoma multiforme. Despite of poor physico-chemical properties of hit compound 1, our medicinal chemistry effort allowed the discovery and characterization of lead compound 33 (SEN461), with improved ADME profile, good bioavailability and active in vitro and in vivo in glioblastoma, gastric and sarcoma tumors., (Copyright © 2015 Elsevier Masson SAS. All rights reserved.)

Published
2015
Full Text
View/download PDF

2. Rational design, synthesis and characterization of potent, non-peptidic Smac mimics/XIAP inhibitors as proapoptotic agents for cancer therapy.

Author

Seneci P, Bianchi A, Battaglia C, Belvisi L, Bolognesi M, Caprini A, Cossu F, Franco Ed, Matteo Md, Delia D, Drago C, Khaled A, Lecis D, Manzoni L, Marizzoni M, Mastrangelo E, Milani M, Motto I, Moroni E, Potenza D, Rizzo V, Servida F, Turlizzi E, Varrone M, Vasile F, and Scolastico C

Subjects
Antineoplastic Agents chemistry, Antineoplastic Agents toxicity, Apoptosis Regulatory Proteins, Bridged Bicyclo Compounds chemical synthesis, Bridged Bicyclo Compounds toxicity, Cell Line, Tumor, Computer Simulation, Crystallography, X-Ray, Drug Design, Drug Screening Assays, Antitumor, Humans, Intracellular Signaling Peptides and Proteins metabolism, Mitochondrial Proteins metabolism, Protein Structure, Tertiary, Structure-Activity Relationship, X-Linked Inhibitor of Apoptosis Protein chemistry, X-Linked Inhibitor of Apoptosis Protein metabolism, Antineoplastic Agents chemical synthesis, Bridged Bicyclo Compounds chemistry, Intracellular Signaling Peptides and Proteins chemistry, Mitochondrial Proteins chemistry, Neoplasms drug therapy, X-Linked Inhibitor of Apoptosis Protein antagonists & inhibitors
Abstract

Novel proapoptotic Smac mimics/IAPs inhibitors have been designed, synthesized and characterized. Computational models and structural studies (crystallography, NMR) have elucidated the SAR of this class of inhibitors, and have permitted further optimization of their properties. In vitro characterization (XIAP BIR3 and linker-BIR2-BIR3 binding, cytotox assays, early ADMET profiling) of the compounds has been performed, identifying one lead for further in vitro and in vivo evaluation.

Published
2009
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results