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Your search keyword '"Raffa, Demetrio"' showing total 13 results
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13 results on '"Raffa, Demetrio"'

1. Pyrazolo[3,4-d]pyrimidine derivatives as COX-2 selective inhibitors: synthesis and molecular modelling studies

Author

RAFFA, Demetrio, MAGGIO, Benedetta, PLESCIA, Fabiana, CASCIOFERRO, Stella Maria, RAIMONDI, Maria Valeria, PLESCIA, Salvatore, CUSIMANO, Maria Grazia, Raffa, D, Maggio, B, Plescia, F, Cascioferro, SM, Raimondi, MV, Plescia, S, and Cusimano, MG

Subjects
Models, Molecular, Sulfonamides, Sheep, Cyclooxygenase 2 Inhibitors, Indomethacin, Anti-Inflammatory Agents, Settore CHIM/08 - Chimica Farmaceutica, Structure-Activity Relationship, 4(3H)-Quinazolinone, Pyrimidines, Docking, Pyrazolo[3,4-d]pyrimidine, Cyclooxygenase 1, Animals, Humans, Pyrazoles, Computer Simulation, COX-2 inhibitor, Nitrobenzenes
Abstract

The pyrazolo[3,4-d]pyrimidine system shows a multitude of interesting pharmacological properties. Owing to the potential anti-inflammatory activity of 5-benzamido-pyrazolo[3,4-d]pyrimidin- 4-one derivatives and considering the easy synthesis of this class of compounds, a set of new 5- benzamido-1H-pyrazolo[3,4-d]pyrimidin-4-ones has been prepared in 42-80% yields by reacting 5- aminopyrazole-4(N-benzoyl)carbohydrazide derivatives and the opportune triethylorthoesters. Compounds 8a, b, 10a–d, and 11a, b revealed a superior inhibitory profile against COX-2, when compared to that of reference standards NS398 and indomethacin. Molecular modelling studies confirmed the obtained biological results.

Published
2009

12. Novel 4-(3-phenylpropionamido), 4-(2-phenoxyacetamido) and 4-(cinnamamido) substituted benzamides bearing the pyrazole or indazole nucleus: synthesis, biological evaluation and mechanism of action

Author

Marianna Lauricella, Giuseppe Daidone, Fabiana Plescia, Antonella D'Anneo, Benedetta Maggio, Demetrio Raffa, Raffa, Demetrio, D'Anneo, Antonella, Plescia, Fabiana, Daidone, Giuseppe, Lauricella, Marianna, and Maggio, Benedetta

Subjects
Indazoles, Stereochemistry, Antineoplastic Agents, Apoptosis, TRAIL-receptor, Pyrazole, 01 natural sciences, Biochemistry, chemistry.chemical_compound, Downregulation and upregulation, Cell Line, Tumor, 2-(3-phenylpropanamido)benzamide, Drug Discovery, medicine, Humans, Moiety, Molecular Biology, Cell Proliferation, Biological evaluation, P53, Indazole, 010405 organic chemistry, Drug Discovery3003 Pharmaceutical Science, 2-cinnamamidobenzamide, Organic Chemistry, Apoptosi, 2-(2-phenoxyacetamido)benzamide, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, medicine.anatomical_structure, Proto-Oncogene Proteins c-bcl-2, Mechanism of action, chemistry, Benzamides, Pyrazoles, Drug Screening Assays, Antitumor, medicine.symptom, Nucleus
Abstract

Based on some common structural features of known compounds interfering with p53 pathways and our previously synthesized benzamides, we synthesized new ethyl 5-(4-substituted benzamido)-1-phenyl-1H-pyrazole-4-carboxylates 26a-c, ethyl 5-(4-substituted benzamido)-1-(pyridin-2-yl)-1H-pyrazole-4-carboxylates 27a-c and N-(1H-indazol-6-yl)-4-substituted benzamides 31a,b bearing in the 4 position of the benzamido moiety the 2-phenylpropanamido or 2-phenoxyacetamido or cinnamamido groups. A preliminary test to evaluate the antiproliferative activity against human lung carcinoma H292 cells highlighted how compound 26c showed the best activity. This last was therefore selected for further studies with the aim to find the mechanism of action. Compound 26c induces intrinsic apoptotic pathway by activating p53 and is also able to activate TRAIL-inducing death pathway by promoting increase of DR4 and DR5 death receptors, downregulation of c-FLIPL and caspase-8 activation.

Published
2019

13. 4-(3H)-quinazolinones N-3 substituted with a five membered heterocycle: A promising scaffold towards bioactive molecules

Author

Demetrio Raffa, Fabiana Plescia, Benedetta Maggio, Giuseppe Daidone, Plescia, Fabiana, Maggio, Benedetta, Daidone, Giuseppe, and Raffa, Demetrio

Subjects
Scaffold, Nitrogen, Bioactive molecules, Anti-Inflammatory Agents, Antitubercular Agents, chemistry.chemical_element, Antineoplastic Agents, 01 natural sciences, Antioxidants, 03 medical and health sciences, chemistry.chemical_compound, Anti-Infective Agents, Drug Discovery, Animals, Humans, Molecule, Benzothiazoles, Quinazolinone, Quinazolinones, 030304 developmental biology, Pharmacology, 0303 health sciences, Molecular Structure, 010405 organic chemistry, Organic Chemistry, N-3 substituted-4-(3H)-quinazolinones, five membered heterocycle, bioactive system, General Medicine, Settore CHIM/08 - Chimica Farmaceutica, Sulfur, Combinatorial chemistry, Bronchodilator Agents, 0104 chemical sciences, Oxygen, Thiazoles, Oxygen atom, chemistry, Anticonvulsants
Abstract

The quinazolinone nucleus represents, among the class of fused heterocycles, a very important scaffold to obtain molecules with biological activities. A review of literature revealed how such kind of fused heterocycles, coming from natural or synthetic source, are associated with a wide range of biological activities. This review is mainly directed towards the 4-(3H)-quinazolinones N-3 substituted with a five membered heterocycle in which all the possible combinations of nitrogen, sulfur and oxygen atoms are present.

Published
2021

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