Search Results - "BERIA, Italo"

Identification of 4,5-Dihydro-1H-pyrazolo[4,3-h]quinazoline Derivatives as a New Class of Orally and Selective Polo-Like Kinase 1 Inhibitors by Beria, Italo, Ballinari, Dario, Bertrand, Jay Aaron, Borghi, Daniela, Bossi, Roberto Tiberio, Brasca, Maria Gabriella, Cappella, Paolo, Caruso, Michele, Ceccarelli, Walter, Ciavolella, Antonella, Cristiani, Cinzia, Croci, Valter, De Ponti, Anna, Fachin, Gabriele, Ferguson, Ronald Dale, Lansen, Jacqueline, Moll, Jurgen Karl, Pesenti, Enrico, Posteri, Helena, Perego, Rita, Rocchetti, Maurizio, Storici, Paola, Volpi, Daniele, Valsasina, Barbara

“…Polo-like kinase 1 (Plk1) is a fundamental regulator of mitotic progression whose overexpression is often associated with oncogenesis and therefore is…”
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Syntheses of brostallicin starting from distamycin A by Beria, Italo, Nesi, Marcella

“…Two syntheses of brostallicin, a DNA minor groove binder now undergoing phase II studies, starting from distamycin A are described. One approach is based upon…”
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Synthesis and Antitumor Activity of New Benzoheterocyclic Derivatives of Distamycin A by Baraldi, Pier Giovanni, Romagnoli, Romeo, Beria, Italo, Cozzi, Paolo, Geroni, Cristina, Mongelli, Nicola, Bianchi, Nicoletta, Mischiati, Carlo, Gambari, Roberto

“…The design, synthesis, and in vivo and in vitro antileukemic activity of a novel series of compounds (13−22 and 34), in which different benzoheterocyclic…”
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Abstract 2810: Computationally predicted sensitivity of clinical cohorts identifies drug relationships and biomarkers associated with response to PCM-075, a PLK1 selective inhibitor by Whitley, Penn, Croucher, Peter J., Valsasina, Barbara, Ballinari, Dario, Beria, Italo, Miner, Jeffrey N., Erlander, Mark G.

“…Abstract Polo-like kinase 1 (PLK1) is a serine-threonine kinase which regulates various cellular processes, including mitosis, DNA replication, and the stress…”
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NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies by Valsasina, Barbara, Beria, Italo, Alli, Cristina, Alzani, Rachele, Avanzi, Nilla, Ballinari, Dario, Cappella, Paolo, Caruso, Michele, Casolaro, Alessia, Ciavolella, Antonella, Cucchi, Ulisse, De Ponti, Anna, Felder, Eduard, Fiorentini, Francesco, Galvani, Arturo, Gianellini, Laura M, Giorgini, Maria L, Isacchi, Antonella, Lansen, Jaqueline, Pesenti, Enrico, Rizzi, Simona, Rocchetti, Maurizio, Sola, Francesco, Moll, Jürgen

“…Polo-like kinase 1 (PLK1) is a serine/threonine protein kinase considered to be the master player of cell-cycle regulation during mitosis. It is indeed…”
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NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor by Beria, Italo, Bossi, Roberto T, Brasca, Maria Gabriella, Caruso, Michele, Ceccarelli, Walter, Fachin, Gabriele, Fasolini, Marina, Forte, Barbara, Fiorentini, Francesco, Pesenti, Enrico, Pezzetta, Daniele, Posteri, Helena, Scolaro, Alessandra, Depaolini, Stefania Re, Valsasina, Barbara

“…As part of our drug discovery effort, we identified and developed 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as PLK1 inhibitors. We now report the…”
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Identification of 4,5-Dihydro-1 H -pyrazolo[4,3- h ]quinazoline Derivatives as a New Class of Orally and Selective Polo-Like Kinase 1 Inhibitors by Beria, Italo, Ballinari, Dario, Bertrand, Jay Aaron, Borghi, Daniela, Bossi, Roberto Tiberio, Brasca, Maria Gabriella, Cappella, Paolo, Caruso, Michele, Ceccarelli, Walter, Ciavolella, Antonella, Cristiani, Cinzia, Croci, Valter, De Ponti, Anna, Fachin, Gabriele, Ferguson, Ronald Dale, Lansen, Jacqueline, Moll, Jurgen Karl, Pesenti, Enrico, Posteri, Helena, Perego, Rita, Rocchetti, Maurizio, Storici, Paola, Volpi, Daniele, Valsasina, Barbara

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Abstract 734: Thienoindoles: New highly promising agents for antibody-drug conjugates generation by Caruso, Michele, Gasparri, Fabio, Valsasina, Barbara, Albanese, Clara, Beria, Italo, Candiani, Ilaria, Ciomei, Marina, Colombo, Nicoletta, Cribioli, Sabrina, Cucchi, Ulisse, Felder, Eduard, Fraietta, Ivan, Galvani, Arturo, Isacchi, Antonella, Marsiglio, Aurelio, Orsini, Paolo, Perego, Rita, Rizzi, Simona, Tomasi, Attilio, Troiani, Sonia, Visco, Carlo, Donati, Daniele

“…Abstract Thienoindoles are a new proprietary class of highly potent DNA minor groove alkylating agents. This class is characterized by a fused thiophene ring…”
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Phosphorylation of TCTP as a Marker for Polo-like Kinase-1 Activity In Vivo by CUCCHI, Ulisse, GIANELLINI, Laura M, GIORGINI, Maria L, CAPPELLA, Paolo, BERIA, Italo, VALSASINA, Barbara, DE PONTI, Anna, SOLA, Francesco, ALZANI, Rachele, PATTON, Veronica, PEZZONI, Alice, TROIANI, Sonia, SACCARDO, Maria B, RIZZI, Simona

“…Polo-like kinase 1 (PLK1) is the master regulator of mitosis and a target for anticancer therapy. To develop a marker of PLK1 activity in cells and tumour…”
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Abstract A149: NMS-P945, a highly active payload for antibody drug conjugates generation by Gasparri, Fabio, Caruso, Michele, Beria, Italo, Colombo, Nicoletta, Orsini, Paolo, Perego, Rita, Rizzi, Simona, Cucchi, Ulisse, Troiani, Sonia, Riccardi Sirtori, Federico, Albanese, Clara, Marsiglio, Aurelio, Fraietta, Ivan, Sola, Francesco, Ciomei, Marina, Cribioli, Sabrina, Visco, Carlo, Felder, Eduard Rudolf, Isacchi, Antonella, Pesenti, Enrico, Galvani, Arturo, Donati, Daniele, Valsasina, Barbara

“…Abstract Antibody-drug conjugates (ADCs) are increasingly employed in different oncology settings with more than forty products in clinical evaluation at…”
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5-(2-Amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors by Caruso, Michele, Valsasina, Barbara, Ballinari, Dario, Bertrand, Jay, Brasca, Maria Gabriella, Caldarelli, Marina, Cappella, Paolo, Fiorentini, Francesco, Gianellini, Laura M., Scolaro, Alessandra, Beria, Italo

“…Synthesis of two new chemical classes of compounds with good PLK1 activity was reported. Crystal structure, enzymatic activity and in vitro cell proliferation…”
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Role of Glutathione Transferases in the Mechanism of Brostallicin Activation by Pezzola, Silvia, Antonini, Giovanni, Geroni, Cristina, Beria, Italo, Colombo, Maristella, Broggini, Massimo, Mongelli, Nicola, Leboffe, Loris, MacArthur, Robert, Mozzi, Alessia Francesca, Federici, Giorgio, Caccuri, Anna Maria

“…Brostallicin is a novel and unique glutathione transferase-activated pro-drug with promising anticancer activity, currently in phase I and II clinical…”
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Abstract 822: Thienoindoles, a novel class of DNA minor groove alkylating agents highly suited for the generation of novel antibody drug conjugates (ADCs) by Valsasina, Barbara, Gasparri, Fabio, Beria, Italo, Colombo, Nicoletta, Orsini, Paolo, Perego, Rita, Rizzi, Simona, Cucchi, Ulisse, Albanese, Clara, Marsiglio, Aurelio, Fraietta, Ivan, Ciomei, Marina, Cribioli, Sabrina, Visco, Carlo, Felder, Eduard R., Isacchi, Antonella, Pesenti, Enrico A., Galvani, Arturo, Donati, Daniele, Caruso, Michele

“…Abstract The rapidly growing field of Antibody-Drug Conjugates (ADCs) has recently spurred the study of novel drug payloads. In particular, much interest has…”
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4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors by Beria, Italo, Valsasina, Barbara, Brasca, Maria Gabriella, Ceccarelli, Walter, Colombo, Maristella, Cribioli, Sabrina, Fachin, Gabriele, Ferguson, Ronald D., Fiorentini, Francesco, Gianellini, Laura M., Giorgini, Maria L., Moll, Jurgen K., Posteri, Helena, Pezzetta, Daniele, Roletto, Fulvia, Sola, Francesco, Tesei, Dania, Caruso, Michele

“…A 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline series of Polo-like kinase inhibitors is reported and the SAR disclosed. The series led to low nanomolar PLK1…”
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5-(2-Amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridi n -4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors by Caruso, Michele, Valsasina, Barbara, Ballinari, Dario, Bertrand, Jay, Brasca, Maria Gabriella, Caldarelli, Marina, Cappella, Paolo, Fiorentini, Francesco, Gianellini, Laura M, Scolaro, Alessandra, Beria, Italo

“…The discovery and characterization of two new chemical classes of potent and selective Polo-like kinase 1 (PLK1) inhibitors is reported. For the most…”
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Correction to Role of Glutathione Transferases in the Mechanism of Brostallicin Activation by Pezzola, Silvia, Antonini, Giovanni, Geroni, Cristina, Beria, Italo, Colombo, Maristella, Broggini, Massimo, Marchini, Sergio, Mongelli, Nicola, Leboffe, Loris, MacArthur, Robert, Mozzi, Alessia Francesca, Federici, Giorgio, Caccuri, Anna Maria

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Cytotoxic α-Halogenoacrylic Derivatives of Distamycin A and Congeners by Beria, Italo, Baraldi, Pier Giovanni, Cozzi, Paolo, Caldarelli, Marina, Geroni, Cristina, Marchini, Sergio, Mongelli, Nicola, Romagnoli, Romeo

“…The mechanism of action of many antitumor agents involves DNA damage, either by direct binding of the drug to DNA or to DNA-binding proteins. However, most of…”
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NMS-P937, a 4,5-dihydro-1 H-pyrazolo[4,3- h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor by Beria, Italo, Bossi, Roberto T., Brasca, Maria Gabriella, Caruso, Michele, Ceccarelli, Walter, Fachin, Gabriele, Fasolini, Marina, Forte, Barbara, Fiorentini, Francesco, Pesenti, Enrico, Pezzetta, Daniele, Posteri, Helena, Scolaro, Alessandra, Depaolini, Stefania Re, Valsasina, Barbara

“…Lead optimization work on the 4,5-dihydro-1 H-pyrazolo[4,3- h]quinazoline series led to identification of NMS-P937. Crystal structure of NMS-P937 with PLK1 was…”
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Cinnamoyl nitrogen mustard derivatives of pyrazole analogues of tallimustine modified at the amidino moiety: design, synthesis, molecular modeling and antitumor activity studies by Baraldi, Pier Giovanni, Beria, Italo, Cozzi, Paolo, Geroni, Cristina, Espinosa, Antonio, Gallo, Miguel A, Entrena, Antonio, Bingham, John P, Hartley, John A, Romagnoli, Romeo

“…The design, synthesis and in vitro activities of a series of cinnamoyl nitrogen mustard pyrazole analogues of tallimustine 8– 13, in which the amidino moiety…”
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Synthesis and growth inhibition activity of α-Bromoacrylic heterocyclic and benzoheterocyclic derivatives of distamycin A modified on the amidino moiety by Baraldi, Pier Giovanni, Beria, Italo, Cozzi, Paolo, Bianchi, Nicoletta, Gambari, Roberto, Romagnoli, Romeo

“…The design, synthesis and in vitro activities of novel α-bromoacryloyl pyrazole, imidazole and benzoheterocyclic derivatives of distamycin A, in which the…”
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