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3 results on '"Cusimano MG"'

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

2. Pyrazolobenzotriazinone derivatives as COX inhibitors: synthesis, biological activity, and molecular-modeling studies.

Author

Raffa D, Migliara O, Maggio B, Plescia F, Cascioferro S, Cusimano MG, Tringali G, Cannizzaro C, and Plescia F

Subjects
Anti-Inflammatory Agents chemical synthesis, Anti-Inflammatory Agents pharmacology, Celecoxib, Cyclooxygenase 2 Inhibitors chemical synthesis, Humans, Models, Molecular, Pyrazoles, Structure-Activity Relationship, Sulfonamides, Cyclooxygenase 2 Inhibitors chemistry, Triazines pharmacology
Abstract

Pyrazolylbenzotriazinones are endowed with a structural analogy with the COX-2 selective inhibitor celecoxib. Considering that our research group has long been interested in the 3-pyrazolyl-substituted benzotriazinones as anti-inflammatory agents, six new pyrazolylbenzotriazinone derivatives 16a-c and 18a-c have been prepared by reacting the opportune ethyl 5-(2-aminobenzamido)-1-(pyridin-2-yl)-1H-pyrazole-4-carboxylate or 5-(2-aminobenzamido)-1-(pyridin-2-yl)-1H-pyrazole-4-carboxyic acid with sodium nitrite in glacial acetic acid. The biological studies revealed a good pharmacological profile for some pyrazolylbenzotriazinones and, in the case of the ethyl 5-(4-oxo-1,2,3-benzotriazin-3(4H)-yl)-1-pyridin-2-yl-1H-pyrazole-4-carboxylate, a good COX-1/COX-2 selectivity. Molecular modeling studies confirmed the obtained biological results.

Published
2010
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3. N-(indazolyl)benzamido derivatives as CDK1 inhibitors: design, synthesis, biological activity, and molecular docking studies.

Author

Raffa D, Maggio B, Cascioferro S, Raimondi MV, Daidone G, Plescia S, Schillaci D, Cusimano MG, Titone L, Colomba C, and Tolomeo M

Subjects
Antineoplastic Agents pharmacology, Benzamides pharmacology, Binding Sites, CDC2 Protein Kinase chemistry, Cell Proliferation drug effects, Cyclin B antagonists & inhibitors, Drug Design, Drug Screening Assays, Antitumor, Humans, Imidazoles pharmacology, K562 Cells, Protein Binding, Structure-Activity Relationship, Antineoplastic Agents chemical synthesis, Benzamides chemical synthesis, CDC2 Protein Kinase antagonists & inhibitors, Imidazoles chemical synthesis, Models, Molecular
Abstract

A series of N-1H-indazole-1-carboxamides has been synthesized and their effects on both CDK1/cyclin B and the K-562 (human chronic myelogenus leukemia) cell line were evaluated. Using a computational model, we have observed that all the most active compounds 9e, f, i-n exhibited the same binding mode of purvanalol A in the ATP-binding cleft. Although they were able to moderately inhibit the leukemic cell line K-562 and to show inhibitory activity against the Cdc2-Cyclin B kinase in the low micromolar range, they turned out to be non-cytotoxic against HuDe (IZSL) primary cell cultures from human derm. These preliminary results are quite encouraging in view of the low toxicity demonstrated by the above-mentioned compounds.

Published
2009
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