List of works - Marco Radi

4-Amino-Substituted Pyrazolo[3,4-d]Pyrimidines: Synthesis and Biological Properties

A Domino Microwave-Assisted Protocol for the Synthesis of 2,6-Disubstituted Pyrimidinones

A Versatile Route to C-6 Arylmethyl-FunctionalizedS-DABO and Related Analogues

scientific article published on 11 July 2007

A cascade screening approach for the identification of Bcr-Abl myristate pocket binders active against wild type and T315I mutant

scientific article published on 18 June 2016

A combination strategy to inhibit Pim-1: synergism between noncompetitive and ATP-competitive inhibitors.

scientific article published on March 2013

A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin

scientific article

A combined targeted/phenotypic approach for the identification of new antiangiogenics agents active on a zebrafish model: from in silico screening to cyclodextrin formulation

scientific article

A convergent approach for the synthesis of ara-neplanocin a analogues under subzero microwave assisted conditions

scientific article published in May 2009

A microwave-assisted multicomponent protocol for the synthesis of benzofuran-2-carboxamides

A multicomponent pharmacophore fragment-decoration approach to identify selective LRRK2-targeting probes

A multidisciplinary approach for the identification of novel HIV-1 non-nucleoside reverse transcriptase inhibitors: S-DABOCs and DAVPs

scientific article

A one-pot two-step microwave-assisted synthesis of N1-substituted 5,6-ring-fused 2-pyridones

A one-pot, two-step microwave-assisted synthesis of highly functionalized benzoxazoles using solid-supported reagents (SSRs)

ATP-competitive inhibitors of mTOR: an update.

scientific article published on January 2011

An alternative synthetic approach for the synthesis of biologically relevant 1,4-disubstituted pyrazolo[3,4-d]pyrimidines

Arylation of 2-Furyl 4-Fluorophenyl Ketone: An Extension of Heck Chemistry towards Novel Integrase Inhibitors

Biologically driven synthesis of pyrazolo[3,4-d]pyrimidines as protein kinase inhibitors: an old scaffold as a new tool for medicinal chemistry and chemical biology studies

scientific article published on 29 May 2014

C6-unsubstituted pyrazolo[3,4-d]pyrimidines are dual Src/Abl inhibitors effective against imatinib mesylate resistant chronic myeloid leukemia cell lines

scientific article

CYP-dependent metabolism of antitumor pyrazolo[3,4-d]pyrimidine derivatives is characterized by an oxidative dechlorination reaction.

scientific article

Combining X-ray crystallography and molecular modeling toward the optimization of pyrazolo[3,4-d]pyrimidines as potent c-Src inhibitors active in vivo against neuroblastoma

scientific article

Computational techniques are valuable tools for the discovery of protein-protein interaction inhibitors: the 14-3-3σ case

scientific article

Cover Feature: Identification of Broad-Spectrum Dengue/Zika Virus Replication Inhibitors by Functionalization of Quinoline and 2,6-Diaminopurine Scaffolds (ChemMedChem 14/2018)

scholarly article by Suzanne J. F. Kaptein et al published 18 July 2018 in ChemMedChem

Crystal structure of HIV-1 reverse transcriptase bound to a non-nucleoside inhibitor with a novel mechanism of action

scientific article

Design and synthesis of thiadiazoles and thiazoles targeting the Bcr-Abl T315I mutant: from docking false positives to ATP-noncompetitive inhibitors

scientific article published in August 2010

Design, synthesis, and biological evaluation of pyrazolo[3,4-d]pyrimidines active in vivo on the Bcr-Abl T315I mutant.

scientific article

Design, synthesis, biological activity, and ADME properties of pyrazolo[3,4-d]pyrimidines active in hypoxic human leukemia cells: a lead optimization study.

scientific article

Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents

scientific article

Discovery of Multitarget Agents Active as Broad-Spectrum Antivirals and Correctors of Cystic Fibrosis Transmembrane Conductance Regulator for Associated Pulmonary Diseases

scientific article

Discovery of Multitarget Antivirals Acting on Both the Dengue Virus NS5-NS3 Interaction and the Host Src/Fyn Kinases

scientific article published on 15 June 2015

Discovery of Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase Competing with the Nucleotide Substrate

article

Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants

scientific article

Discovery of the first small molecule inhibitor of human DDX3 specifically designed to target the RNA binding site: towards the next generation HIV-1 inhibitors.

scientific article

Dual Src and Abl inhibitors target wild type Abl and the AblT315I Imatinib-resistant mutant with different mechanisms

scientific article published on 18 April 2010

Exploring the chemical space around the privileged pyrazolo[3,4-d]pyrimidine scaffold: toward novel allosteric inhibitors of T315I-mutated Abl.

scientific article

HIV-1 RT Inhibitors with a Novel Mechanism of Action: NNRTIs that Compete with the Nucleotide Substrate

scientific article

Homology Modeling, Validation and Dynamics of the G Protein-coupled Estrogen Receptor 1 (GPER-1).

scientific article

Identification of Breast Cancer Inhibitors Specific for G Protein-Coupled Estrogen Receptor (GPER)-Expressing Cells.

scientific article published on 18 May 2017

Identification of broad-spectrum dengue/Zika virus replication inhibitors by functionalization of quinoline and 2,6-diaminopurine scaffolds.

scientific article

Identification of potent c-Src inhibitors strongly affecting the proliferation of human neuroblastoma cells.

scientific article

In vitro optimization of non-small cell lung cancer activity with troxacitabine, L-1,3-dioxolane-cytidine, prodrugs

scientific article

Insight into the allosteric inhibition of Abl kinase

scientific article published on 8 May 2014

Microwave-Assisted Acylation of Amines, Alcohols, and Phenols by the Use of Solid-Supported Reagents (SSRs)

scientific article published on 01 November 2004

Microwave-Assisted Domino Reactions of Propargylamines with Isothiocyanates: Selective Synthesis of 2-Aminothiazoles and 2-Amino-4-methylenethiazolines

Microwave-assisted organocatalytic multicomponent Knoevenagel/hetero Diels–Alder reaction for the synthesis of 2,3-dihydropyran[2,3-c]pyrazoles

Microwave-enhanced Sonogashira coupling reaction of substituted pyrimidinones and pyrimidine nucleosides

Molecular characterization of c-Abl/c-Src kinase inhibitors targeted against murine tumour progenitor cells that express stem cell markers

scientific article

Multitarget CFTR Modulators Endowed with Multiple Beneficial Side Effects for Cystic Fibrosis Patients: Toward a Simplified Therapeutic Approach †

scientific article published on 03 December 2019

New insights into small-molecule inhibitors of Bcr-Abl

scientific article published on January 2011

Parallel solution-phase synthesis of 4-dialkylamino-2-methylsulfonyl-6-vinylpyrimidines

scientific article published in January 2005

Practical one-pot two-step protocol for the microwave-assisted synthesis of highly functionalized rhodanine derivatives

scientific article published in January 2010

Preclinical discovery and development of maraviroc for the treatment of HIV.

scientific article published on 30 April 2015

Pyrazolo[3,4-d]pyrimidine Prodrugs: Strategic Optimization of the Aqueous Solubility of Dual Src/Abl Inhibitors

scientific article published on 20 May 2013

Recent highlights in the synthesis of highly functionalized pyrimidines

scientific article published on 12 June 2009

Rethinking the old antiviral drug moroxydine: Discovery of novel analogues as anti-hepatitis C virus (HCV) agents

scientific article published on 12 September 2015

SRC kinase inhibitors: an update on patented compounds.

scientific article published on January 2011

Scaffold Morphing Approach To Expand the Toolbox of Broad-Spectrum Antivirals Blocking Dengue/Zika Replication

scientific article published on 23 January 2019

Solid-phase synthesis (SPS) of substituted uracils via Oxone® cleavage methodology

Studies on the ATP Binding Site of Fyn Kinase for the Identification of New Inhibitors and Their Evaluation as Potential Agents against Tauopathies and Tumors

scientific article published on 29 April 2015

Synthesis and biological evaluation of new enantiomerically pure azole derivatives as inhibitors of Mycobacterium tuberculosis.

scientific article

Synthesis of an Original Oxygenated Taxuspine X Analogue: a Versatile “Non-Natural” Natural Product with Remarkable P-gp Modulating Activity

scientific article published on 01 May 2008

Synthesis of enantiomerically pure α-[4-(1-substituted)-1,2,3-triazol-4-yl]-benzylacetamides via microwave-assisted click chemistry: towards new potential antimicrobial agents

Synthesis of reactive cytidine derivatives as building blocks for cross-linking oligonucleotides

Synthesis, Biological Activity, and ADME Properties of Novel S-DABOs/N-DABOs as HIV Reverse Transcriptase Inhibitors

article

Synthesis, biological evaluation and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis.

scientific article published on 7 August 2008

Synthesis, biological evaluation, and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis: part 2. Synthesis of rigid pyrazolones.

scientific article

Toward the discovery of novel anti-HIV drugs. Second-generation inhibitors of the cellular ATPase DDX3 with improved anti-HIV activity: synthesis, structure-activity relationship analysis, cytotoxicity studies, and target validation.

scientific article published on 22 June 2011

Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies

scientific article

Troxacitabine prodrugs for pancreatic cancer.

scientific article published on January 2007

Unconventional plasticity of HIV-1 reverse transcriptase: how inhibitors could open a connection "gate" between allosteric and catalytic sites

scientific article published on 25 November 2013

Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors

scientific article published on 6 November 2012

List of works by Marco Radi

4-Amino-Substituted Pyrazolo[3,4-d]Pyrimidines: Synthesis and Biological Properties

A Domino Microwave-Assisted Protocol for the Synthesis of 2,6-Disubstituted Pyrimidinones

A Versatile Route to C-6 Arylmethyl-FunctionalizedS-DABO and Related Analogues

A cascade screening approach for the identification of Bcr-Abl myristate pocket binders active against wild type and T315I mutant

A combination strategy to inhibit Pim-1: synergism between noncompetitive and ATP-competitive inhibitors.

A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin

A combined targeted/phenotypic approach for the identification of new antiangiogenics agents active on a zebrafish model: from in silico screening to cyclodextrin formulation

A convergent approach for the synthesis of ara-neplanocin a analogues under subzero microwave assisted conditions

A microwave-assisted multicomponent protocol for the synthesis of benzofuran-2-carboxamides

A multicomponent pharmacophore fragment-decoration approach to identify selective LRRK2-targeting probes

A multidisciplinary approach for the identification of novel HIV-1 non-nucleoside reverse transcriptase inhibitors: S-DABOCs and DAVPs

A one-pot two-step microwave-assisted synthesis of N1-substituted 5,6-ring-fused 2-pyridones

A one-pot, two-step microwave-assisted synthesis of highly functionalized benzoxazoles using solid-supported reagents (SSRs)

ATP-competitive inhibitors of mTOR: an update.

An alternative synthetic approach for the synthesis of biologically relevant 1,4-disubstituted pyrazolo[3,4-d]pyrimidines

Arylation of 2-Furyl 4-Fluorophenyl Ketone: An Extension of Heck Chemistry towards Novel Integrase Inhibitors

Biologically driven synthesis of pyrazolo[3,4-d]pyrimidines as protein kinase inhibitors: an old scaffold as a new tool for medicinal chemistry and chemical biology studies

C6-unsubstituted pyrazolo[3,4-d]pyrimidines are dual Src/Abl inhibitors effective against imatinib mesylate resistant chronic myeloid leukemia cell lines

CYP-dependent metabolism of antitumor pyrazolo[3,4-d]pyrimidine derivatives is characterized by an oxidative dechlorination reaction.

Combining X-ray crystallography and molecular modeling toward the optimization of pyrazolo[3,4-d]pyrimidines as potent c-Src inhibitors active in vivo against neuroblastoma

Computational techniques are valuable tools for the discovery of protein-protein interaction inhibitors: the 14-3-3σ case

Cover Feature: Identification of Broad-Spectrum Dengue/Zika Virus Replication Inhibitors by Functionalization of Quinoline and 2,6-Diaminopurine Scaffolds (ChemMedChem 14/2018)

Crystal structure of HIV-1 reverse transcriptase bound to a non-nucleoside inhibitor with a novel mechanism of action

Design and synthesis of thiadiazoles and thiazoles targeting the Bcr-Abl T315I mutant: from docking false positives to ATP-noncompetitive inhibitors

Design, synthesis, and biological evaluation of pyrazolo[3,4-d]pyrimidines active in vivo on the Bcr-Abl T315I mutant.

Design, synthesis, biological activity, and ADME properties of pyrazolo[3,4-d]pyrimidines active in hypoxic human leukemia cells: a lead optimization study.

Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents

Discovery of Multitarget Agents Active as Broad-Spectrum Antivirals and Correctors of Cystic Fibrosis Transmembrane Conductance Regulator for Associated Pulmonary Diseases

Discovery of Multitarget Antivirals Acting on Both the Dengue Virus NS5-NS3 Interaction and the Host Src/Fyn Kinases

Discovery of Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase Competing with the Nucleotide Substrate

Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants

Discovery of the first small molecule inhibitor of human DDX3 specifically designed to target the RNA binding site: towards the next generation HIV-1 inhibitors.

Dual Src and Abl inhibitors target wild type Abl and the AblT315I Imatinib-resistant mutant with different mechanisms

Exploring the chemical space around the privileged pyrazolo[3,4-d]pyrimidine scaffold: toward novel allosteric inhibitors of T315I-mutated Abl.

HIV-1 RT Inhibitors with a Novel Mechanism of Action: NNRTIs that Compete with the Nucleotide Substrate

Homology Modeling, Validation and Dynamics of the G Protein-coupled Estrogen Receptor 1 (GPER-1).

Identification of Breast Cancer Inhibitors Specific for G Protein-Coupled Estrogen Receptor (GPER)-Expressing Cells.

Identification of broad-spectrum dengue/Zika virus replication inhibitors by functionalization of quinoline and 2,6-diaminopurine scaffolds.

Identification of potent c-Src inhibitors strongly affecting the proliferation of human neuroblastoma cells.

In vitro optimization of non-small cell lung cancer activity with troxacitabine, L-1,3-dioxolane-cytidine, prodrugs

Insight into the allosteric inhibition of Abl kinase

Microwave-Assisted Acylation of Amines, Alcohols, and Phenols by the Use of Solid-Supported Reagents (SSRs)

Microwave-Assisted Domino Reactions of Propargylamines with Isothiocyanates: Selective Synthesis of 2-Aminothiazoles and 2-Amino-4-methylenethiazolines

Microwave-assisted organocatalytic multicomponent Knoevenagel/hetero Diels–Alder reaction for the synthesis of 2,3-dihydropyran[2,3-c]pyrazoles

Microwave-enhanced Sonogashira coupling reaction of substituted pyrimidinones and pyrimidine nucleosides

Molecular characterization of c-Abl/c-Src kinase inhibitors targeted against murine tumour progenitor cells that express stem cell markers

Multitarget CFTR Modulators Endowed with Multiple Beneficial Side Effects for Cystic Fibrosis Patients: Toward a Simplified Therapeutic Approach †

New insights into small-molecule inhibitors of Bcr-Abl

Parallel solution-phase synthesis of 4-dialkylamino-2-methylsulfonyl-6-vinylpyrimidines

Practical one-pot two-step protocol for the microwave-assisted synthesis of highly functionalized rhodanine derivatives

Preclinical discovery and development of maraviroc for the treatment of HIV.

Pyrazolo[3,4-d]pyrimidine Prodrugs: Strategic Optimization of the Aqueous Solubility of Dual Src/Abl Inhibitors

Recent highlights in the synthesis of highly functionalized pyrimidines

Rethinking the old antiviral drug moroxydine: Discovery of novel analogues as anti-hepatitis C virus (HCV) agents

SRC kinase inhibitors: an update on patented compounds.

Scaffold Morphing Approach To Expand the Toolbox of Broad-Spectrum Antivirals Blocking Dengue/Zika Replication

Solid-phase synthesis (SPS) of substituted uracils via Oxone® cleavage methodology

Studies on the ATP Binding Site of Fyn Kinase for the Identification of New Inhibitors and Their Evaluation as Potential Agents against Tauopathies and Tumors

Synthesis and biological evaluation of new enantiomerically pure azole derivatives as inhibitors of Mycobacterium tuberculosis.

Synthesis of an Original Oxygenated Taxuspine X Analogue: a Versatile “Non-Natural” Natural Product with Remarkable P-gp Modulating Activity

Synthesis of enantiomerically pure α-[4-(1-substituted)-1,2,3-triazol-4-yl]-benzylacetamides via microwave-assisted click chemistry: towards new potential antimicrobial agents

Synthesis of reactive cytidine derivatives as building blocks for cross-linking oligonucleotides

Synthesis, Biological Activity, and ADME Properties of Novel S-DABOs/N-DABOs as HIV Reverse Transcriptase Inhibitors

Synthesis, biological evaluation and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis.

Synthesis, biological evaluation, and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis: part 2. Synthesis of rigid pyrazolones.

Toward the discovery of novel anti-HIV drugs. Second-generation inhibitors of the cellular ATPase DDX3 with improved anti-HIV activity: synthesis, structure-activity relationship analysis, cytotoxicity studies, and target validation.

Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies

Troxacitabine prodrugs for pancreatic cancer.

Unconventional plasticity of HIV-1 reverse transcriptase: how inhibitors could open a connection "gate" between allosteric and catalytic sites

Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors