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List of works by Sandro Cosconati

3-(Fur-2-yl)-10-(2-phenylethyl)-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one, a novel adenosine receptor antagonist with A(2A)-mediated neuroprotective effects

scientific article

3-aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one: a novel template for the design of highly selective A₂B adenosine receptor antagonists

scientific article published on 7 February 2012

4-Imidazo[2,1-b]thiazole-1,4-DHPs and neuroprotection: preliminary study in hits searching

scientific article published on 04 March 2019

4-Substituted Benzenesulfonamides Incorporating Bi/Tricyclic Moieties Act as Potent and Isoform-Selective Carbonic Anhydrase II/IX Inhibitors

scientific article published on 27 June 2018

A balance between elongation and trimming regulates telomere stability in stem cells

scientific journal article

A conformationally frozen peptoid boosts CXCR4 affinity and anti-HIV activity

scientific article published on 3 July 2012

A more detailed picture of the interactions between virtual screening-derived hits and the DNA G-quadruplex: NMR, molecular modelling and ITC studies

scientific article published on 30 May 2011

A unique capsular polysaccharide structure from the psychrophilic marine bacterium Colwellia psychrerythraea 34H that mimics antifreeze (glyco)proteins

scientific article

Antiproliferative and proapoptotic activity of CLM3, a novel multiple tyrosine kinase inhibitor, alone and in combination with SN-38 on endothelial and cancer cells

scientific article published on April 2011

Architecture of the Human Urotensin II Receptor: Comparison of the Binding Domains of Peptide and Non-Peptide Urotensin II Agonists

scientific article published on 01 April 2005

Architecture of the Human Urotensin II Receptor: Comparison of the Binding Domains of Peptide and Non-Peptide Urotensin II Agonists

Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase

scientific article

Benzofuroxane Derivatives as Multi-Effective Agents for the Treatment of Cardiovascular Diabetic Complications. Synthesis, Functional Evaluation, and Molecular Modeling Studies

scientific article published on November 20, 2012

Best Matching Protein Conformations and Docking Programs for a Virtual Screening Campaign Against SMO Receptor.

scientific article

Boosting Fmoc Solid-Phase Peptide Synthesis by Ultrasonication

scientific article published on 30 July 2019

Characterization of 2,4-Diamino-6-oxo-1,6-dihydropyrimidin-5-yl Ureido Based Inhibitors of Trypanosoma brucei FolD and Testing for Antiparasitic Activity

scientific article

Characterizing the 1,4-dihydropyridines binding interactions in the L-type Ca2+ channel: model construction and docking calculations

scientific article published on 3 March 2007

Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity

scientific article published on 18 September 2017

Conformational Control of Integrin-Subtype Selectivity in isoDGR Peptide Motifs: A Biological Switch

scientific article published on 01 November 2010

Decoration of Chondroitin Polysaccharide with Threonine: Synthesis, Conformational Study, and Ice-Recrystallization Inhibition Activity.

scientific article published on 26 June 2017

Deepening the Topology of the Translocator Protein Binding Site by Novel N,N-Dialkyl-2-arylindol-3-ylglyoxylamides

scientific article published on 28 July 2015

Design, synthesis, and biological evaluation of novel 2-((2-(4-(substituted)phenylpiperazin-1-yl)ethyl)amino)-5'-N-ethylcarboxamidoadenosines as potent and selective agonists of the A2A adenosine receptor

scientific article published on 25 March 2015

Design, synthesis, and functionalization of dimeric peptides targeting chemokine receptor CXCR4.

scientific article published on 11 October 2011

Development of Novel Peptide-Based Michael Acceptors Targeting Rhodesain and Falcipain-2 for the Treatment of Neglected Tropical Diseases (NTDs).

scientific article

Development of novel 1,4-benzodiazepine-based Michael acceptors as antitrypanosomal agents

scientific article published on 21 June 2016

Discovery of N-aryl-naphthylamines as in vitro inhibitors of the interaction between HIV integrase and the cofactor LEDGF/p75.

scientific article published on 22 June 2015

Discovery of Pyrido[3',2':5,6]thiopyrano[4,3-d]pyrimidine-Based Antiproliferative Multikinase Inhibitors

scientific article published on 17 January 2019

Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure

scientific article published on 26 February 2019

Discovery of the first dual G-triplex/G-quadruplex stabilizing compound: a new opportunity in the targeting of G-rich DNA structures?

scientific article

Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer

scientific article published on 8 August 2017

Elucidation of the enantioselective recognition mechanism of a penicillin G acylase-based chiral stationary phase towards a series of 2-aryloxy-2-arylacetic acids

scientific article published on 01 August 2006

Endogenous vs Exogenous Allosteric Modulators in GPCRs: A dispute for shuttling CB1 among different membrane microenvironments

scientific article

Ensemble-Docking Approach on BACE-1: Pharmacophore Perception and Guidelines for Drug Design

scholarly article by Vittorio Limongelli et al published 11 June 2007 in ChemMedChem

Ensemble-docking approach on BACE-1: pharmacophore perception and guidelines for drug design

scientific article published in May 2007

Exploiting the 4-Phenylquinazoline Scaffold for the Development of High Affinity Fluorescent Probes for the Translocator Protein (TSPO).

scientific article

Exploring the chemical space of G-quadruplex binders: discovery of a novel chemotype targeting the human telomeric sequence

scientific article published on 27 November 2013

Exploring the molecular basis of the enantioselective binding of penicillin G acylase towards a series of 2-aryloxyalkanoic acids: a docking and molecular dynamics study

scientific article published on 8 August 2006

From the pharmacophore to the homology model of the benzodiazepine receptor: the indolyglyoxylamides affair

scientific article published on January 2012

Homology modeling of NR2B modulatory domain of NMDA receptor and analysis of ifenprodil binding

scientific article published on October 2007

Human recombinant beta-secretase immobilized enzyme reactor for fast hits' selection and characterization from a virtual screening library

scientific article

Identification of 5-arylidene-4-thiazolidinone derivatives endowed with dual activity as aldose reductase inhibitors and antioxidant agents for the treatment of diabetic complications

scientific article published on 08 April 2011

Identification of anxiolytic/nonsedative agents among indol-3-ylglyoxylamides acting as functionally selective agonists at the gamma-aminobutyric acid-A (GABAA) alpha2 benzodiazepine receptor.

scientific article published in June 2009

Identification of highly conserved residues involved in inhibition of HIV-1 RNase H function by Diketo acid derivatives

scientific article

Identification of novel molecular scaffolds for the design of MMP-13 inhibitors: A first round of lead optimization

article

Imidazo[2,1-b]thiazole system: a scaffold endowing dihydropyridines with selective cardiodepressant activity

scientific article

Increasing αvβ3 selectivity of the anti-angiogenic drug cilengitide by N-methylation.

scientific article

Inhibition of Histone Demethylases LSD1 and UTX Regulates ERα Signaling in Breast Cancer

scientific article published on 16 December 2019

Inhibition of ocular aldose reductase by a new benzofuroxane derivative ameliorates rat endotoxic uveitis

scientific article

Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2.

scientific article published on 14 August 2015

Lead Discovery of Dual G-Quadruplex Stabilizers and Poly(ADP-ribose) Polymerases (PARPs) Inhibitors: A New Avenue in Anticancer Treatment.

scientific article

Lead Optimization of 2-Phenylindolylglyoxylyldipeptide Murine Double Minute (MDM)2/Translocator Protein (TSPO) Dual Inhibitors for the Treatment of Gliomas.

scientific article

Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity

scientific article published on 9 May 2013

Modeling of Cdc25B Dual Specifity Protein Phosphatase Inhibitors: Docking of Ligands and Enzymatic Inhibition Mechanism

article

Monothiocarbamates Strongly Inhibit Carbonic Anhydrases in Vitro and Possess Intraocular Pressure Lowering Activity in an Animal Model of Glaucoma

scientific article published on 2 June 2016

N-Substituted Quinolinonyl Diketo Acid Derivatives as HIV Integrase Strand Transfer Inhibitors and Their Activity against RNase H Function of Reverse Transcriptase

scientific article

New 2-heterocyclyl-imidazo[2,1-i]purin-5-one derivatives as potent and selective human A3 adenosine receptor antagonists

scientific article published on 28 June 2011

New insights in the structure-activity relationships of 2-phenylamino-substituted benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors

scientific article published on 7 March 2018

New insights into the interaction between pyrrolyl diketoacids and HIV-1 integrase active site and comparison with RNase H.

scientific article

New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors

scientific article

Novel 2-substituted-benzimidazole-6-sulfonamides as carbonic anhydrase inhibitors: synthesis, biological evaluation against isoforms I, II, IX and XII and molecular docking studies

scientific article published on 01 December 2019

Novel N2-substituted pyrazolo[3,4-d]pyrimidine adenosine A3 receptor antagonists: inhibition of A3-mediated human glioblastoma cell proliferation.

scientific article published on May 2010

Optimization Strategy of Novel Peptide-Based Michael Acceptors for the Treatment of Human African Trypanosomiasis

scientific article published on 27 November 2019

Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors

scientific article published on 16 September 2013

Progresses in the pursuit of aldose reductase inhibitors: The structure-based lead optimization step

scientific article published on 05 March 2012

Properly substituted analogues of BIX-01294 lose inhibition of G9a histone methyltransferase and gain selective anti-DNA methyltransferase 3A activity

scientific article

Protein flexibility in virtual screening: the BACE-1 case study

scientific article

Pursuing Aldose Reductase Inhibitors through in Situ Cross-Docking and Similarity-Based Virtual Screening

scientific article published on 01 September 2009

Revisiting a receptor-based pharmacophore hypothesis for human A(2A) adenosine receptor antagonists

scientific article published on 20 June 2013

Sampling protein motion and solvent effect during ligand binding

scientific article published on 11 January 2012

Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells

scientific article published on 15 January 2014

Shading the TRF2 Recruiting Function: A New Horizon in Drug Development

article

Shooting for Selective Druglike G-Quadruplex Binders: Evidence for Telomeric DNA Damage and Tumor Cell Death

article

Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations

scientific article published in February 2009

Src inhibitors act through different mechanisms in Non-Small Cell Lung Cancer models depending on EGFR and RAS mutational status

scientific article

State-of-the-art methodologies for the discovery and characterization of DNA G-quadruplex binders.

scientific article published on January 2012

Structural and conformational requisites in DNA quadruplex groove binding: another piece to the puzzle

scientific article

Structure-Activity Relationship Studies on Oxazolo[3,4-<i>a</i>]pyrazine Derivatives Leading to the Discovery of a Novel Neuropeptide S Receptor Antagonist with Potent <i>In Vivo</i> Activity

scientific article published on 18 March 2021

Structure-activity relationship of the exopolysaccharide from a psychrophilic bacterium: A strategy for cryoprotection

scientific article (publication date: 20 January 2017)

Structure-activity relationship refinement and further assessment of 4-phenylquinazoline-2-carboxamide translocator protein ligands as antiproliferative agents in human glioblastoma tumors

scientific article published on 17 March 2014

Structure-based virtual screening and biological evaluation of Mycobacterium tuberculosis adenosine 5'-phosphosulfate reductase inhibitors

scientific article published on 15 October 2008

Studies on enantioselectivity of chiral 4-acetylamino-6-alkyloxy-2-alkylthiopyrimidines acting as antagonists of the human A adenosine receptor

scientific article published on 09 November 2017

Switchable Protecting Strategy for Solid Phase Synthesis of DNA and RNA Interacting Nucleopeptides.

scientific article

Synthesis and biological evaluation of 4-phenylquinazoline-2-carboxamides designed as a novel class of potent ligands of the translocator protein

scientific article

Synthesis and biological evaluation of CTP synthetase inhibitors as potential agents for the treatment of African trypanosomiasis

scientific article published on 2 August 2012

Synthesis and biological evaluation of novel peptidomimetics as rhodesain inhibitors

scientific article published on 16 November 2015

Synthesis and gene silencing properties of siRNAs containing terminal amide linkages

scientific article

Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators

scientific article published on 26 June 2013

Tailoring a lead-like compound targeting multiple G-quadruplex structures

scientific article published on 27 November 2018

Tandem Application of Virtual Screening and NMR Experiments in the Discovery of Brand New DNA Quadruplex Groove Binders

scientific article published in 2009

Tandem application of ligand-based virtual screening and G4-OAS assay to identify novel G-quadruplex-targeting chemotypes.

scientific article

The First Sphingosine 1-Phosphate Lyase Inhibitors against Multiple Sclerosis: A Successful Drug Discovery Tale

scientific article published on 10 June 2014

The G-Triplex DNA

Tuning RNA Interference by Enhancing siRNA/PAZ Recognition

scientific article

Unbinding of Translocator Protein 18 kDa (TSPO) Ligands: From in Vitro Residence Time to in Vivo Efficacy via in Silico Simulations

scientific article published on 03 July 2019

Virtual Screening with AutoDock: Theory and Practice

scientific article

Water-soluble pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines as human A₃ adenosine receptor antagonists

scientific article published on 18 May 2012

tert-Butylcarbamate-containing histone deacetylase inhibitors: apoptosis induction, cytodifferentiation, and antiproliferative activities in cancer cells

scientific article published on 25 March 2013