Search

Your search keyword '"Cristiana Costantini"' showing total 2 results
Start Over Author "Cristiana Costantini"
2 results on '"Cristiana Costantini"'

1. Inhibition of activated STAT5 in Bcr/Abl expressing leukemia cells with new pimozide derivatives

Author

Stefania Grimaudo, Riccardo Baruchello, Maria Meli, Riccardo Rondanin, Romeo Romagnoli, Manlio Tolomeo, Paolo Marchetti, Giacomo Padroni, Sara Fochi, Rosaria Maria Pipitone, Daniele Simoni, Cristiana Costantini, Rondanin,R, Simoni, D, Romagnoli, R, Baruchello,R, Marchetti,P, Costantini, C, Fochi, S, Padroni,G, Grimaudo, S, Pipitone, RM, Meli, M, and Tolomeo, M

Subjects
Clinical Biochemistry, Fusion Proteins, bcr-abl, Pharmaceutical Science, Apoptosis, Biochemistry, Settore MED/15 - Malattie Del Sangue, Cell Line, Structure-Activity Relationship, Pimozide, Settore BIO/13 - Biologia Applicata, hemic and lymphatic diseases, Drug Discovery, medicine, STAT5 Transcription Factor, Cytotoxic T cell, Humans, Phosphorylation, Molecular Biology, Transcription factor, STAT5, Cell Proliferation, biology, Dose-Response Relationship, Drug, Molecular Structure, Chemistry, STAT5 inhibitors,Pimozide,BCR/ABL expressing leukemia, Apoptosis,Cell growth inhibition, Organic Chemistry, Cell Cycle, medicine.disease, Settore CHIM/08 - Chimica Farmaceutica, Leukemia, Cancer research, biology.protein, Settore BIO/14 - Farmacologia, Molecular Medicine, K562 Cells, medicine.drug, Chronic myelogenous leukemia
Abstract

STATs are transcription factors acting as intracellular signaling after stimulation with cytokines, growth factors and hormones. STAT5 is also constitutively active in many forms of cancers, including chronic myelogenous leukemia, acute lymphoblastic leukemia and Hodgkin's lymphoma. Recently, literature reported that the neuroleptic drug pimozide inhibits STAT5 phosphorylation inducing apoptosis in CML cells. We undertook an investigation from pimozide structure, obtaining simple derivatives with cytotoxic and STAT5-inhibitory activity, two of them markedly more potent than pimozide.

Published
2014

2. 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors

Author

Riccardo Rondanin, Maria Meli, Paolo Marchetti, Gianfranco Battistuzzi, Cristiana Costantini, Daniele Simoni, Valeria Carollo, Giuseppe Giannini, Stefania Mangiola, Loredana Vesci, Riccardo Baruchello, Tiziana Brunetti, Walter Cabri, Manlio Tolomeo, Baruchello, R, Simoni, D, Marchetti, P, Rondanin, R, Mangiola, S, Costantini, C, Meli, M, Giannini, G, Vesci, L, Carollo, V, Brunetti, T, Battistuzzi, G, Tolomeo, M, Cabri W, Baruchello R., Simoni D., Marchetti P., Rondanin R., Mangiola S., Costantini C, Meli M., Giannini G, Vesci L., Carollo V., Brunetti T., Battistuzzi G., and Tolomeo M.

Subjects
Spectrometry, Mass, Electrospray Ionization, Magnetic Resonance Spectroscopy, medicine.drug_class, Stereochemistry, Pyridines, Carboxamide, Apoptosis, Resorcinol, Anti-cancer drugs, chemistry.chemical_compound, Residue (chemistry), Amide, Drug Discovery, Heat shock protein 90, Anti-cancer drugs, 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]- pyridines, medicine, Cytotoxic T cell, Humans, Heat shock protein 90, HSP90 Heat-Shock Proteins, Pharmacology, Hydroxamic acid, Chemistry, Cell growth, Organic Chemistry, General Medicine, Nuclear magnetic resonance spectroscopy, 4 5 6 7-Tetrahydro-isoxazolo-[4 5-c]-pyridines, Flow Cytometry, Settore CHIM/08 - Chimica Farmaceutica, hsp90, Settore BIO/14 - Farmacologia, K562 Cells, Cell Division
Abstract

Hsp90 is considered an interesting therapeutic target for anticancer drug development. Here we describe a new class of 4,5,6,7-tetrahydro-isoxazolo-[4,5-c]-pyridine compounds. A small library of derivatives has been synthesized and investigated. Some reported compounds show interesting properties combining both notable binding to Hsp90 and potent cell growth inhibitory activity. N-5 substitution with a 2,4 resorcinol carboxamide appears crucial for activity. Moreover, a derivative bearing a hydroxamic acid residue bound to C-3 amide portion was found to inhibit both Hsp90 and HDAC6.

Published
2013

Catalog

Books, media, physical & digital resources
See catalog results