Roberto Di Santo


Titolo Pubblicato in Anno
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
Recent advances in recovery of lycopene from tomato waste. A potent antioxidant with endless benefits MOLECULES 2021
Toxicological aspects of cannabinoid, pesticide and metal levels detected in light Cannabis inflorescences grown in Italy FOOD AND CHEMICAL TOXICOLOGY 2021
Small-molecule inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H function. Challenges and recent developments CURRENT MEDICINAL CHEMISTRY 2021
New pyrimidine and pyridine derivatives as multitarget cholinesterase inhibitors. Design, synthesis, and in vitro and in cellulo evaluation ACS CHEMICAL NEUROSCIENCE 2021
Salmonella typhimurium and pseudomonas aeruginosa respond differently to the fe chelator deferiprone and to some novel deferiprone derivatives INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES 2021
Discovery of a pyrimidine compound endowed with antitumor activity INVESTIGATIONAL NEW DRUGS 2020
New deferiprone derivatives as multi-functional cholinesterase inhibitors. Design, synthesis and in vitro evaluation EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 2020
Pyrrolyl pyrazoles as non-diketo acid inhibitors of the HIV-1 ribonuclease H function of reverse transcriptase ACS MEDICINAL CHEMISTRY LETTERS 2020


  • PE5_18


  • 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.




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)



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

© Università degli Studi di Roma "La Sapienza" - Piazzale Aldo Moro 5, 00185 Roma