Roberto Di Santo

Pubblicazioni

Titolo Pubblicato in Anno
Inhibition of Leishmania infantum Trypanothione Reductase by New Aminopropanone Derivatives Interacting with the NADPH Binding Site MOLECULES 2023
Pyrrolyl and indolyl α-γ-diketo acid derivatives acting as selective inhibitors of human carbonic anhydrases IX and XII PHARMACEUTICALS 2023
Plants and Small Molecules: An Up-and-Coming Synergy PLANTS 2023
Synergistic Effects of Caffeine in Combination with Conventional Drugs: Perspectives of a Drug That Never Ages PHARMACEUTICALS 2023
Effects of Modified Glucosamine on the Chondrogenic Potential of Circulating Stem Cells under Experimental Inflammation INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES 2023
Diketo acid inhibitors of nsp13 of SARS-CoV-2 block viral replication ANTIVIRAL RESEARCH 2023
Role of a Novel Heparanase Inhibitor on the Balance between Apoptosis and Autophagy in U87 Human Glioblastoma Cells CELLS 2023
Miconazole-like Scaffold is a Promising Lead for Naegleria fowleri-Specific CYP51 Inhibitors JOURNAL OF MEDICINAL CHEMISTRY 2023
Evaluation of the Anti-Histoplasma capsulatum activity of Indole and Nitrofuran derivatives and their pharmacological safety in three-dimensional cell cultures PHARMACEUTICS 2022
Design, synthesis, and In vitro, in silico and in cellulo evaluation of new Pyrimidine and Pyridine amide and Carbamate derivatives as multi-functional Cholinesterase Inhibitors PHARMACEUTICALS 2022
Ultrastructural damages to H1N1 influenza virus caused by vapor essential oils MOLECULES 2022
New Inhibitors of the Human p300/CBP Acetyltransferase Are Selectively Active against the Arabidopsis HAC Proteins INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES 2022
Acetylcholinesterase inhibitors for the treatment of Alzheimer’s disease–a patent review (2016–present) EXPERT OPINION ON THERAPEUTIC PATENTS 2021
Design, synthesis and biological evaluation of new pyrimidine derivatives as anticancer agents MOLECULES 2021
Investigation of Commiphora myrrha (Nees) Engl. Oil and Its Main Components for Antiviral Activity PHARMACEUTICALS 2021
Analytical characterization of an inulin-type fructooligosaccharide from root-tubers of Asphodelus ramosus L PHARMACEUTICALS 2021
Design, synthesis and biological evaluation of a series of iron and copper chelating deferiprone derivatives as new agents active against Candida albicans BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 2021
Anti-tumoral effects of a (1H-pyrrol-1-yl)methyl-1H-benzoimidazole carbamate ester derivative on head and neck squamous carcinoma cell lines PHARMACEUTICALS 2021
Effect of Heparanase inhibitor on Tissue Factor overexpression in platelets and endothelial cells induced by anti-β2-GPI antibodies JOURNAL OF THROMBOSIS AND HAEMOSTASIS 2021
Quinolinonyl non-diketo acid derivatives as Inhibitors of HIV-1 ribonuclease H and polymerase functions of reverse transcriptase JOURNAL OF MEDICINAL CHEMISTRY 2021

ERC

  • PE5_18

KET

  • Life-science technologies & biotechnologies

Interessi di ricerca

Drug Design.

Antimicrobial agents active agains virues  such as HIV, SARSCoV, HCV, CHIKV,

Antibacterial agents based on quinolone scaffold. Metallo-beta-lactamase inhibitors.

Antiprotozoals

Antifungals

Antimycobacterals

Antitumor agenst with specific mechanism of action: Kinase Inhibitors. Inhibitors of tubulin polimerization. Antitumoral agents found by phenotypic approach.

Natural substances: plant extracts for medicinal and nutraceutical applications.

My laboratory is involved in design and synthesis of compounds active against various microbial agents.
We use the most modern synthetic approaches like microwave heating flow chemistry, parallel synthesis,
as well as the classic batch approach to synthesize the designed compounds.
Big expertise in the design and synthesis of compounds active against a number of targets of HIV, HCV, fungi, protozoa and bacteria. Decennial experience in this field led to the discovery of compounds with potent activity against integrase, in particular on the strand transfer step of integration process. The studied started in the last part of 90s, with the discovery of the first group synthetic polyhydroxy aromatic derivatives that inhibited IN activities.  Later, new ADK compounds characterized by a pyrrole and or quinoline ring that were very potent IN inhibitors active in cell-based assays, have been designed and synthesized. Several molecular tools have been designed that contributed to understand the mechanism of action of HIV Integrase. Expertise also in other fields of the medicinal chemistry: antifungal and antiprotozoal agents, compounds active against HCV polymerase, anti-TBC, as well as chemotherapeutic agents useful against liquid and solid tumors.

Several  interaction with Companies, to develop antimalarial agents, ligands of 5-HT receptors, and compounds active against the aggregation of beta-amyloid fibrils:

Project “beta-amiloid” (Sigma-Tau);
“Malaria - Artekin” (Sigma-Tau);
Project “New ligands of 5-HT4 receptors” (ACRAF).
Project “Triamcinolone” (AlfaSigma)
Project Heparanase Inhibitors (AlfaSigma)
Project Combiotic specifications (Pfizer)
Project MBL inhibitors (Microbo)

 

Keywords

drug design and synthesis.
antiviral agents
antibacterial agents
antifungal agents
Antiprotozoal Agents
antimycobacterial agents
antitumor agents
tyrosine kinase inhibitors
tubulin inhibitors

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