List of works - Federico Da Settimo Passetti

2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database searching

scientific article published in December 2005

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)-ones: tricyclic heteroaromatic derivatives as a new class of benzodiazepine receptor ligands

scientific article

3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: a new class of selective A1 adenosine receptor antagonists.

scientific article published on February 2001

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

scientific article published on 27 June 2018

4-amino-6-alkyloxy-2-alkylthiopyrimidine derivatives as novel non-nucleoside agonists for the adenosine A1 receptor

scientific article

5-amino-2-phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one: a versatile scaffold to obtain potent and selective A3 adenosine receptor antagonists.

scientific article published on 10 October 2007

A Virtual Screening Study of the 18 kDa Translocator Protein using Pharmacophore Models Combined with 3D-QSAR Studies

scientific article published on 01 October 2009

A mixed-valence diruthenium(II,III) complex endowed with high stability: from experimental evidence to theoretical interpretation

scientific article published on 13 October 2020

A new approach to control the enigmatic activity of aldose reductase.

scientific article

A novel 2,3-diphenyl-4H-pyrido[1,2-a]pyrimidin-4-one derivative inhibits endothelial cell dysfunction and smooth muscle cell proliferation/activation

scientific article published on 01 December 2013

A1 adenosine receptor antagonists, 3-aryl[1,2,4]triazino[4,3-a]benzimidazol-4-(10H)-ones (ATBIs) andN-alkyl andN-acyl-(7-substituted-2-phenylimidazo[1,2-a][1,3,5]triazin-4-yl)amines (ITAs): Different recognition of bovine and human binding sites

A3 receptor ligands: past, present and future trends

scientific article published on January 2010

Acetic acid aldose reductase inhibitors bearing a five-membered heterocyclic core with potent topical activity in a visual impairment rat model.

scientific article published on 2 May 2008

Adenosine deaminase in the modulation of immune system and its potential as a novel target for treatment of inflammatory disorders.

scientific article published on June 2012

Allosteric modulators for adenosine receptors: an alternative to the orthosteric ligands.

scientific article published on January 2010

Allosteric modulators of human A2B adenosine receptor

scientific article published on 19 December 2013

Antineoplastic activity of the multitarget tyrosine kinase inhibitors CLM3 and CLM94 in medullary thyroid cancer in vitro.

scientific article published on 21 August 2014

Anxiolytic properties of a 2-phenylindolglyoxylamide TSPO ligand: Stimulation of in vitro neurosteroid production affecting GABAA receptor activity

article

Anxiolytic-like effects of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides by modulation of translocator protein promoting neurosteroid biosynthesis

scientific article

Apoptosis therapy in cancer: the first single-molecule co-activating p53 and the translocator protein in glioblastoma.

scientific article published on 23 April 2014

Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation

scientific article

Arylthioamides as H2S Donors: l-Cysteine-Activated Releasing Properties and Vascular Effects in Vitro and in Vivo

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

Benzothiopyranoindole-Based Antiproliferative Agents: Synthesis, Cytotoxicity, Nucleic Acids Interaction, and Topoisomerases Inhibition Properties

scientific article published on 01 September 2009

CLM29 and CLM24, pyrazolopyrimidine derivatives, have antitumoral activity in vitro in anaplastic thyroid cancer, with or without BRAF mutation.

scientific article published on 19 August 2015

CLM29, a multi-target pyrazolopyrimidine derivative, has anti-neoplastic activity in medullary thyroid cancer in vitro and in vivo.

scientific article published on 12 June 2014

CLM3, a multitarget tyrosine kinase inhibitor with antiangiogenic properties, is active against primary anaplastic thyroid cancer in vitro and in vivo.

scientific article published on January 2014

CLM94, a novel cyclic amide with anti-VEGFR-2 and antiangiogenic properties, is active against primary anaplastic thyroid cancer in vitro and in vivo.

scientific article published on 25 January 2012

Computational Studies of Epidermal Growth Factor Receptor: Docking Reliability, Three-Dimensional Quantitative Structure−Activity Relationship Analysis, and Virtual Screening Studies

article

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

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

Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists

scientific article published on 13 February 2008

Derivatives of Benzimidazol-2-ylquinoline and Benzimidazol-2-ylisoquinoline as Selective A1 Adenosine Receptor Antagonists with Stimulant Activity on Human Colon Motility

scientific article published on 27 July 2011

Design, synthesis and biological evaluation of novel N-alkyl- and N-acyl-(7-substituted-2-phenylimidazo[1,2-a][1,3,5]triazin-4-yl)amines (ITAs) as novel A(1) adenosine receptor antagonists

scientific article published in November 2002

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

scientific article published on 17 January 2019

Editorial [Hot Topic:The Indolylglyoxylamide Scaffold as an Useful Tool to Obtain Anxiolytic Agents (Guest Editors: Sabrina Taliani & Federico Da Settimo )]

scientific article published on 01 January 2012

Effects of newly-developed benzodiazepine ligands on noise-induced mitochondrial damage in the rat

scientific article published on 01 July 2000

Enantiomeric 4-Acylamino-6-alkyloxy-2 Alkylthiopyrimidines As Potential A3 Adenosine Receptor Antagonists: HPLC Chiral Resolution and Absolute Configuration Assignment by a Full Set of Chiroptical Spectroscopy.

scientific article published on 20 April 2016

Evaluation of novel N1-methyl-2-phenylindol-3-ylglyoxylamides as a new chemotype of 18 kDa translocator protein-selective ligand suitable for the development of positron emission tomography radioligands

scientific article

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

scientific article

Exploiting the Indole Scaffold to Design Compounds Binding to Different Pharmacological Targets

scientific article published on 16 May 2020

Exploiting the pyrazolo[3,4-d]pyrimidin-4-one ring system as a useful template to obtain potent adenosine deaminase inhibitors

scientific article published in March 2009

Genetic analysis of dTSPO, an outer mitochondrial membrane protein, reveals its functions in apoptosis, longevity, and Ab42-induced neurodegeneration

scientific article

Geometrically constrained analogues of N-benzylindolylglyoxylylamides: [1, 2, 4]triazino[4, 3-a]benzimidazol-4(10H)-one derivatives as potential new ligands at the benzodiazepine receptor.

scientific article published in September 2003

High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives.

scientific article

Highlighting the New Advances in Drug Discovery and Development

article

Hydrogen Sulphide: Biopharmacological Roles in the Cardiovascular System and Pharmaceutical Perspectives ⬇️

scientific article published on January 1, 2012

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

article

Inhibition of adenosine deaminase attenuates inflammation in experimental colitis.

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

scientific article

Long lasting MDM2/Translocator protein modulator: a new strategy for irreversible apoptosis of human glioblastoma cells

scientific article published on 09 January 2016

Long lasting inhibition of Mdm2-p53 interaction potentiates mesenchymal stem cell differentiation into osteoblasts

scientific article published on 28 January 2019

Medicinal chemistry of indolylglyoxylamide GABAA/BzR high affinity ligands: identification of novel anxiolytic/non sedative agents

scientific article published on January 2012

Medicinal chemistry of indolylglyoxylamide TSPO high affinity ligands with anxiolytic-like effects.

scientific article published on January 2012

Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives

scientific article published on 8 September 2013

N'-Phenylindol-3-ylglyoxylohydrazide derivatives: synthesis, structure-activity relationships, molecular modeling studies, and pharmacological action on brain benzodiazepine receptors.

scientific article published in September 1998

N,N-dialkyl-2-phenylindol-3-ylglyoxylamides. A new class of potent and selective ligands at the peripheral benzodiazepine receptor.

scientific article published on March 2004

Naphtho[1,2-d]isothiazole acetic acid derivatives as a novel class of selective aldose reductase inhibitors.

scientific article

New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.

scientific article published on January 2007

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

Non-nucleoside inhibitors of human adenosine kinase: synthesis, molecular modeling, and biological studies.

scientific article published on 14 February 2011

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 N-(arylalkyl)indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor: synthesis, biological evaluation, and molecular modeling analysis of the structure-activity relationships.

scientific article

Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands

scientific article

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

Novel fluorescent triazinobenzimidazole derivatives as probes for labelling human A1 and A2B adenosine receptor subtypes

scientific article published on 01 November 2018

Novel irreversible fluorescent probes targeting the 18 kDa translocator protein: synthesis and biological characterization.

scientific article

Novel positive allosteric modulators of A<sub>2B</sub> adenosine receptor acting as bone mineralisation promoters

scientific article published on 01 December 2021

Novel pyrazolopyrimidine derivatives as tyrosine kinase inhibitors with antitumoral activity in vitro and in vivo in papillary dedifferentiated thyroid cancer.

scientific article published on 8 December 2010

Novel, highly potent adenosine deaminase inhibitors containing the pyrazolo[3,4-d]pyrimidine ring system. Synthesis, structure-activity relationships, and molecular modeling studies.

scientific article published in August 2005

Novel, highly potent aldose reductase inhibitors: cyano(2-oxo-2,3-dihydroindol-3-yl)acetic acid derivatives

scientific article

Osteoblast differentiation and survival: A role for A2B adenosine receptor allosteric modulators

scientific article published on 18 September 2014

PIGA (N,N-Di-n-butyl-5-chloro-2-(4-chlorophenyl)indol-3-ylglyoxylamide), a new mitochondrial benzodiazepine-receptor ligand, induces apoptosis in C6 glioma cells.

scientific article published in June 2005

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

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

scientific article published on 01 September 2009

Pyrido[1,2-a]pyrimidin-4-one Derivatives as a Novel Class of Selective Aldose Reductase Inhibitors Exhibiting Antioxidant Activity

scientific article published on 11 September 2007

Recent advances in the development of dual topoisomerase I and II inhibitors as anticancer drugs.

scientific article

Receptor Tyrosine Kinase Kit and Gastrointestinal Stromal Tumours: An Overview ⬇️

scientific article published on January 1, 2011

Refinement of the benzodiazepine receptor site topology by structure-activity relationships of new N-(heteroarylmethyl)indol-3-ylglyoxylamides

scientific article published on April 2006

Residence Time, a New parameter to Predict Neurosteroidogenic Efficacy of Translocator Protein (TSPO) Ligands: the Case Study of N,N-Dialkyl-2-arylindol-3-ylglyoxylamides

scientific article

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

Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.

scientific article

Spirohydantoin derivatives of thiopyrano[2,3-b]pyridin-4(4H)-one as potent in vitro and in vivo aldose reductase inhibitors.

scientific article published in January 2005

Structural requirements to obtain highly potent and selective 18 kDa Translocator Protein (TSPO) Ligands.

scientific article published on January 2011

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 optimization of tyrosine kinase inhibitor CLM3. Design, synthesis, functional evaluation, and molecular modeling studies

scientific article published on 5 February 2014

Synthesis and benzodiazepine receptor affinity of derivatives of the new tricyclic heteroaromatic system pyrido[3',2':5,6]thiopyrano[4,3-c]pyridazin-3(2H,5H)-one

scientific article published in March 2005

Synthesis and biological evaluation in U87MG glioma cells of (ethynylthiophene)sulfonamido-based hydroxamates as matrix metalloproteinase inhibitors

scientific article published on 2 April 2011

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 evaluation of translocator 18 kDa protein (TSPO) positron emission tomography (PET) radioligands with low binding sensitivity to human single nucleotide polymorphism rs6971.

scientific article

Synthesis andin vitroantiproliferative activity of new substituted benzo[3′,2′:5,6]thiopyrano[4,3-d]pyrimidines

Synthesis, structure-activity relationships, and molecular modeling studies of N-(indol-3-ylglyoxylyl)benzylamine derivatives acting at the benzodiazepine receptor.

scientific article published in December 1996

Synthetic analogues of flavonoids with improved activity against platelet activation and aggregation as novel prototypes of food supplements

scientific article published on 16 December 2014

TSPO PIGA Ligands Promote Neurosteroidogenesis and Human Astrocyte Well-Being

scientific article published on 29 June 2016

TSPO ligand residence time influences human glioblastoma multiforme cell death/life balance.

scientific article

Targeting the 18-kDa translocator protein: recent perspectives for neuroprotection

scientific article published on 03 August 2015

Tertiary amides with a five-membered heteroaromatic ring as new probes for the translocator protein.

scientific article

The Anxiolytic Etifoxine Binds to TSPO Ro5-4864 Binding Site with Long Residence Time Showing a High Neurosteroidogenic Activity

scientific article published on 31 March 2017

Translocator protein ligands as promising therapeutic tools for anxiety disorders

scientific article

Tricyclic Sulfonamides Incorporating Benzothiopyrano[4,3-c]pyrazole and Pyridothiopyrano[4,3-c]pyrazole Effectively Inhibit α- and β-Carbonic Anhydrase: X-ray Crystallography and Solution Investigations on 15 Isoforms

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

[1,2,4]Triazino[4,3-a]benzimidazole acetic acid derivatives: a new class of selective aldose reductase inhibitors.

scientific article published in December 2001

p53 functional inhibitors behaving like pifithrin-β counteract the Alzheimer peptide non-β-amyloid component effects in human SH-SY5Y cells

scientific article published on 28 March 2014

List of works by Federico Da Settimo Passetti

2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database searching

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

3-Aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: tricyclic heteroaromatic derivatives as a new class of benzodiazepine receptor ligands

3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: a new class of selective A1 adenosine receptor antagonists.

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

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

4-amino-6-alkyloxy-2-alkylthiopyrimidine derivatives as novel non-nucleoside agonists for the adenosine A1 receptor

5-amino-2-phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one: a versatile scaffold to obtain potent and selective A3 adenosine receptor antagonists.

A Virtual Screening Study of the 18 kDa Translocator Protein using Pharmacophore Models Combined with 3D-QSAR Studies

A mixed-valence diruthenium(II,III) complex endowed with high stability: from experimental evidence to theoretical interpretation

A new approach to control the enigmatic activity of aldose reductase.

A novel 2,3-diphenyl-4H-pyrido[1,2-a]pyrimidin-4-one derivative inhibits endothelial cell dysfunction and smooth muscle cell proliferation/activation

A1 adenosine receptor antagonists, 3-aryl[1,2,4]triazino[4,3-a]benzimidazol-4-(10H)-ones (ATBIs) andN-alkyl andN-acyl-(7-substituted-2-phenylimidazo[1,2-a][1,3,5]triazin-4-yl)amines (ITAs): Different recognition of bovine and human binding sites

A3 receptor ligands: past, present and future trends

Acetic acid aldose reductase inhibitors bearing a five-membered heterocyclic core with potent topical activity in a visual impairment rat model.

Adenosine deaminase in the modulation of immune system and its potential as a novel target for treatment of inflammatory disorders.

Allosteric modulators for adenosine receptors: an alternative to the orthosteric ligands.

Allosteric modulators of human A2B adenosine receptor

Antineoplastic activity of the multitarget tyrosine kinase inhibitors CLM3 and CLM94 in medullary thyroid cancer in vitro.

Anxiolytic properties of a 2-phenylindolglyoxylamide TSPO ligand: Stimulation of in vitro neurosteroid production affecting GABAA receptor activity

Anxiolytic-like effects of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides by modulation of translocator protein promoting neurosteroid biosynthesis

Apoptosis therapy in cancer: the first single-molecule co-activating p53 and the translocator protein in glioblastoma.

Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation

Arylthioamides as H2S Donors: l-Cysteine-Activated Releasing Properties and Vascular Effects in Vitro and in Vivo

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

Benzothiopyranoindole-Based Antiproliferative Agents: Synthesis, Cytotoxicity, Nucleic Acids Interaction, and Topoisomerases Inhibition Properties

CLM29 and CLM24, pyrazolopyrimidine derivatives, have antitumoral activity in vitro in anaplastic thyroid cancer, with or without BRAF mutation.

CLM29, a multi-target pyrazolopyrimidine derivative, has anti-neoplastic activity in medullary thyroid cancer in vitro and in vivo.

CLM3, a multitarget tyrosine kinase inhibitor with antiangiogenic properties, is active against primary anaplastic thyroid cancer in vitro and in vivo.

CLM94, a novel cyclic amide with anti-VEGFR-2 and antiangiogenic properties, is active against primary anaplastic thyroid cancer in vitro and in vivo.

Computational Studies of Epidermal Growth Factor Receptor: Docking Reliability, Three-Dimensional Quantitative Structure−Activity Relationship Analysis, and Virtual Screening Studies

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

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

Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists

Derivatives of Benzimidazol-2-ylquinoline and Benzimidazol-2-ylisoquinoline as Selective A1 Adenosine Receptor Antagonists with Stimulant Activity on Human Colon Motility

Design, synthesis and biological evaluation of novel N-alkyl- and N-acyl-(7-substituted-2-phenylimidazo[1,2-a][1,3,5]triazin-4-yl)amines (ITAs) as novel A(1) adenosine receptor antagonists

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

Editorial [Hot Topic:The Indolylglyoxylamide Scaffold as an Useful Tool to Obtain Anxiolytic Agents (Guest Editors: Sabrina Taliani & Federico Da Settimo )]

Effects of newly-developed benzodiazepine ligands on noise-induced mitochondrial damage in the rat

Enantiomeric 4-Acylamino-6-alkyloxy-2 Alkylthiopyrimidines As Potential A3 Adenosine Receptor Antagonists: HPLC Chiral Resolution and Absolute Configuration Assignment by a Full Set of Chiroptical Spectroscopy.

Evaluation of novel N1-methyl-2-phenylindol-3-ylglyoxylamides as a new chemotype of 18 kDa translocator protein-selective ligand suitable for the development of positron emission tomography radioligands

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

Exploiting the Indole Scaffold to Design Compounds Binding to Different Pharmacological Targets

Exploiting the pyrazolo[3,4-d]pyrimidin-4-one ring system as a useful template to obtain potent adenosine deaminase inhibitors

Genetic analysis of dTSPO, an outer mitochondrial membrane protein, reveals its functions in apoptosis, longevity, and Ab42-induced neurodegeneration

Geometrically constrained analogues of N-benzylindolylglyoxylylamides: [1, 2, 4]triazino[4, 3-a]benzimidazol-4(10H)-one derivatives as potential new ligands at the benzodiazepine receptor.

High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives.

Highlighting the New Advances in Drug Discovery and Development

Hydrogen Sulphide: Biopharmacological Roles in the Cardiovascular System and Pharmaceutical Perspectives ⬇️

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

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

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

Inhibition of adenosine deaminase attenuates inflammation in experimental colitis.

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

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

Long lasting MDM2/Translocator protein modulator: a new strategy for irreversible apoptosis of human glioblastoma cells

Long lasting inhibition of Mdm2-p53 interaction potentiates mesenchymal stem cell differentiation into osteoblasts

Medicinal chemistry of indolylglyoxylamide GABAA/BzR high affinity ligands: identification of novel anxiolytic/non sedative agents

Medicinal chemistry of indolylglyoxylamide TSPO high affinity ligands with anxiolytic-like effects.

Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives

N'-Phenylindol-3-ylglyoxylohydrazide derivatives: synthesis, structure-activity relationships, molecular modeling studies, and pharmacological action on brain benzodiazepine receptors.

N,N-dialkyl-2-phenylindol-3-ylglyoxylamides. A new class of potent and selective ligands at the peripheral benzodiazepine receptor.

Naphtho[1,2-d]isothiazole acetic acid derivatives as a novel class of selective aldose reductase inhibitors.

New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.

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

Non-nucleoside inhibitors of human adenosine kinase: synthesis, molecular modeling, and biological studies.

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

Novel N-(arylalkyl)indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor: synthesis, biological evaluation, and molecular modeling analysis of the structure-activity relationships.

Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands

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

Novel fluorescent triazinobenzimidazole derivatives as probes for labelling human A1 and A2B adenosine receptor subtypes

Novel irreversible fluorescent probes targeting the 18 kDa translocator protein: synthesis and biological characterization.

Novel positive allosteric modulators of A<sub>2B</sub> adenosine receptor acting as bone mineralisation promoters

Novel pyrazolopyrimidine derivatives as tyrosine kinase inhibitors with antitumoral activity in vitro and in vivo in papillary dedifferentiated thyroid cancer.

Novel, highly potent adenosine deaminase inhibitors containing the pyrazolo[3,4-d]pyrimidine ring system. Synthesis, structure-activity relationships, and molecular modeling studies.

Novel, highly potent aldose reductase inhibitors: cyano(2-oxo-2,3-dihydroindol-3-yl)acetic acid derivatives

Osteoblast differentiation and survival: A role for A2B adenosine receptor allosteric modulators

PIGA (N,N-Di-n-butyl-5-chloro-2-(4-chlorophenyl)indol-3-ylglyoxylamide), a new mitochondrial benzodiazepine-receptor ligand, induces apoptosis in C6 glioma cells.

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