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Role of Glutathione Transferases in the Mechanism of Brostallicin Activation

Autor: Silvia, Pezzola, Giovanni, Antonini, Cristina, Geroni, Italo, Beria, Maristella, Colombo, Massimo, Broggini, Sergio, Marchini, Nicola, Mongelli, Loris, Leboffe, Robert, MacArthur, Alessia Francesca, Mozzi, Giorgio, Federici, Anna Maria, Caccuri

Publikováno v: Biochemistry. 49:226-235

Brostallicin is a novel and unique glutathione transferase-activated pro-drug with promising anticancer activity, currently in phase I and II clinical evaluation. In this work, we show that, in comparison with the parental cell line showing low GST l

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d551619c23702171c412c9b997d576ee
https://doi.org/10.1021/bi901689s

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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

Autor: Jay Bertrand, Dario Ballinari, Paolo Cappella, Michele Caruso, Francesco Fiorentini, Alessandra Scolaro, Italo Beria, Laura Gianellini, Barbara Valsasina, Marina Caldarelli, Maria Gabriella Brasca

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:96-101

The discovery and characterization of two new chemical classes of potent and selective Polo-like kinase 1 (PLK1) inhibitors is reported. For the most interesting compounds, we discuss the biological activities, crystal structures and preliminary phar

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::912628e99927a261c288c2a65d023ede
https://doi.org/10.1016/j.bmcl.2011.11.065

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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

Autor: Roberto Bossi, Daniele Pezzetta, Gabriele Fachin, Barbara Forte, Alessandra Scolaro, Italo Beria, Walter Ceccarelli, Enrico Pesenti, Michele Caruso, Francesco Fiorentini, Stefania Re Depaolini, Marina Fasolini, Helena Posteri, Barbara Valsasina, Maria Gabriella Brasca

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:2969-2974

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 optimization of this class that led to the identification of NMS-P937, a potent, selective a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1eb1c72f2e8179a8a325d3bbb4369e24
https://doi.org/10.1016/j.bmcl.2011.03.054

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Abstract 734: Thienoindoles: New highly promising agents for antibody-drug conjugates generation

Publikováno v: Cancer Research. 78:734-734

Thienoindoles are a new proprietary class of highly potent DNA minor groove alkylating agents. This class is characterized by a fused thiophene ring whose intrinsic electron-withdrawing character provides a nearly optimal increase in stability and po

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d034ee8d17eb4a7b7e70715e1089086e
https://doi.org/10.1158/1538-7445.am2018-734

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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

Autor: Jeffrey N. Miner, Peter J. P. Croucher, Penn Whitley, Dario Ballinari, Barbara Valsasina, Italo Beria, Mark G. Erlander

Publikováno v: Cancer Research. 78:2810-2810

Polo-like kinase 1 (PLK1) is a serine-threonine kinase which regulates various cellular processes, including mitosis, DNA replication, and the stress response, and is over-expressed in many malignancies. PCM-075, a PLK1 selective inhibitor, is curren

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c8d8ca996c4c2e43cc1f3c6547c334f0
https://doi.org/10.1158/1538-7445.am2018-2810

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Syntheses of brostallicin starting from distamycin A

Autor: Marcella Nesi, Italo Beria

Publikováno v: Tetrahedron Letters. 43:7323-7327

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 the selective hydrolysis via imide activation of the C-terminus amide. Besides employing tr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::72330218c56a18e52a8f5aed3ba55956
https://doi.org/10.1016/s0040-4039(02)01733-1

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Cytotoxic alpha-Bromoacrylic derivatives of low molecular weight

Autor: Benedetta Reinach, Cristina Geroni, Nicola Mongelli, Marina Caldarelli, Luisella Vignati, Italo Beria, Paolo Cozzi

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 12:1467-1471

In vitro and in vivo activities of a small series of alpha-bromoacrylic derivatives of low molecular weight (MW) are described and compared with those of alpha-bromoacrylic derivatives of distamycin-like frames. Low MW compounds, when lacking of a st

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a54ab17c50e36b347d7137380070f971
https://doi.org/10.1016/s0960-894x(02)00177-4

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Synthesis and Antitumor Activity of New Benzoheterocyclic Derivatives of Distamycin A

Autor: Mongelli N, Cristina Geroni, Pier Giovanni Baraldi, Roberto Gambari, Paolo Cozzi, Nicoletta Bianchi, Italo Beria, Carlo Mischiati, Romeo Romagnoli

Publikováno v: Journal of Medicinal Chemistry. 43:2675-2684

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 rings, bearing a nitrogen mustard or a benzoyl nitrogen mustard or an alpha-bromoacryloyl group

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5c56fb19d867cdef6a603d257ce3e553
https://doi.org/10.1021/jm9911229

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