Prof. Domenico Spinelli

Graduated cum laude in Chemistry (1955, Bari), Assistant Professor of Organic Chemistry (1956, Bari; 1962, Genova), full Professor of Organic Chemistry and of Physical Organic Chemistry (1968, Sassari; 1969, Palermo; 1974, Bologna).

Official appointments

President of the Division of Organic Chemistry (1993-1995) of the SCI, Vice-President (1996-1998), President (1999-2001) and past-President (2002-2004) of the Italian Chemical Society. Member of the Executive Committee of FECS (2002-2004). In 1974 he received the golden “Sigillum Magnum” of the University of Palermo. Recipient of the “A. Mangini” (1996) and of “D. Marotta” (2003) golden awards and of the golden Sigillum of the Italian Chemical Society (2007). He is Honorary Lifetime Member of the Indian Society of Chemists and Biologists (2005) “in recognition of outstanding contributions in the field of Chemical Sciences, Drug development and promotion of Scientific understanding”, awarded with Diploma of International Scientific Partnership Foundation (Moscow) “for outstanding achievements in heterocyclic chemistry”, and recipient of the Medal “In memory of Professor Kost” for 2007 instituted by ISPF and the Russian Chemical Society. National Scientific Coordinator of several projects (PRIN and FIRB) supported by the MIUR. Scientific Coeditor of “Topics in Heterocyclic Systems” and of “Targets in Heterocyclic Systems”. For long time Coordinator of the “Dottorato di Ricerca in Scienze Farmaceutiche” at the University of Bologna. Member of several Scientific Society. Member of the European Academy of Sciences and Arts.

Scientific activity

Author of more than three hundred papers on the study of the reactivity and properties of five membered heterocycles [thiophenes and benzothiophenes (nucleophilic aromatic substitutions); 1,2,4-oxadiazoles and isoxazoles (mononuclear rearrangements of heterocycles); nitrosoimidazoles and condensed nitrosoimidazoles (ring-ring interconversions); 1,3,4-oxadiazoles, -thiadiazoles and thiazoles (decarboxylation reactions); furans and cogeners (enolization reactions); etc.], of micellar catalysis, of the mutagenic properties of nitroderivatives, of the properties of carnitine and its derivatives, of the pharmacological properties of thiazinooxadiazolones and of 1,4-diaryl-2,3-dinitro-1,3-butadienes, of theoretical DFT computations on chemical and biological models, etc..

The two principal lines of research have been: 1) the study of the course and of the mechanism of SNAr processes, especially in thiophenes and benzo[b]thiophenes; 2) the study of ring-ring interconversions of azoles.

Concerning the first line particular attention has been devoted to the examination of steric effects in five-membered ring derivatives, to the application of linear free energy relationships, to the study of the intimate mechanism of base catalysis and of the course of some base-assisted abnormal (i.e. with rearrangement) nucleophilic substitutions on 3-bromo-2-nitrobenzo[b]thiophene. Recently some efforts have been devoted to the use of ring-opening products of nitrothiophenes as building blocks for synthetic applications and as anti-cancer agents.

Concerning the second line efforts have been specially targeted to a deep insight into the mechanism of the mononuclear rearrangement of heterocycles for which many facets have been investigated (for example, the different kinds of catalysis occurring, the effect of the structure of the starting and final heterocycles as well as of the side chain on both reactivity and mechanism). Recently very promising results have been collected by using data from ab-initio calculations to enlighten the course of the studied reactions as well as of enzymatic mechanism.

Finally a re-examination of the Cusmano-Ruccia reaction has been carried out studying its course on several condensed nitrosoimidazoles. Interestingly this last project has furnished products with promising biological activity as calcium entry blockers.

Incursions in medicinal chemistry have furnished also promising results in the field of anticancer drugs and very recently in that of agents reverting MDR.

Invited Lectures

Selective Ligands for Actinide-Lanthanide Separations
Design, Synthesis, And Pharmacological Properties Of New Cb₂ Cannabinoid Receptor Ligands
Novel Rearrangements in Targeted Synthesis of Natural Compound Analogs
Nef-Isocyanide Adducts as key Intermediates for Synthesis of Heterocyclic Compounds
Multicomponent 1,3-Dipolar Cycloadditions of Stabilized Azomethine Ylides
Discovering new applications of chiral N-sulfinyl imines in heterocyclic chemistry
Aliphatic Nitrocompounds as Strategic Sources of Heterocycles
Synthetic Strategies for New Pyrazoles of Potential Biological Activities
Enaminones in the synthesis of heterocyclic systems. [2+2] Cycloadditions, ring expansion reactions and other transformations
Design, synthesis and pharmacological properties of new thiazole and thiadiazole derivatives
Cultivating over thirty years the passion to build heterocycles from 1,2-diaza-1,3-dienes
[1,4]Thiazino[3,4-c][1,2,4]oxadiazol-3-ones: an examination of their reactivity and of their biological profile
Effective Conversion of Carbohydrate Molecules to Nitrogen-containing Heterocyclic Derivatives
Recent Advances in Appel Salt Chemistry
Heterocyclic compounds in the design of biodegradable polymers
Synthesis and study of some triazolo Isoxazole heterocyclic Compounds
Three different approaches to target the T315I mutation: ATP-competitive, ATP-non-competitive and 14-3-3 inhibitors
Tetrapyrrolic macrocycles: Synthetic features and potential applications
Reactivity of alpha-halogen substituted pyridinium ylides.
Benzopyran building blocks: herald of hope for multitarget drug discovery
A new general 3CR leading to 1,4,5-trisubstituted-1,2,3-triazoless
Marine alkaloid nortopsentin analogues inhibitors of cyclin-dependent kinase 1 (CDK1)