Search Results - "Fallacara, Anna Lucia"
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An Update on JAK Inhibitors
Published in Current medicinal chemistry (01-01-2019)“…Janus kinases (JAKs) are a family of non-receptor tyrosine kinases, composed by four members, JAK1, JAK2, JAK3 and TYK2. JAKs are involved in different…”
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Pyrrolo[2,3-d]Pyrimidines as Kinase Inhibitors
Published in Current medicinal chemistry (01-06-2017)“…The pyrrolo[2,3-d]pyrimidine nucleus is a deaza-isostere of adenine, the nitrogenous base of ATP, and is present in many ATP-competitive inhibitors of…”
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Optimization of Aminoimidazole Derivatives as Src Family Kinase Inhibitors
Published in Molecules (Basel, Switzerland) (17-09-2018)“…Protein kinases have emerged as crucial targets for cancer therapy over the last decades. Since 2001, 40 and 39 kinase inhibitors have been approved by FDA and…”
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The Pyrazolo[3,4- d ]Pyrimidine Derivative Si306 Encapsulated into Anti-GD2-Immunoliposomes as Therapeutic Treatment of Neuroblastoma
Published in Biomedicines (12-03-2022)“…Si306, a pyrazolo[3,4- ]pyrimidine derivative recently identified as promising anticancer agent, has shown favorable in vitro and in vivo activity profile…”
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Probing the Binding Site of Abl Tyrosine Kinase Using in Situ Click Chemistry
Published in ACS medicinal chemistry letters (14-02-2013)“…Modern combinatorial chemistry is used to discover compounds with desired function by an alternative strategy, in which the biological target is directly…”
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Efficient optimization of pyrazolo[3,4-d]pyrimidines derivatives as c-Src kinase inhibitors in neuroblastoma treatment
Published in Bioorganic & medicinal chemistry letters (15-11-2018)“…[Display omitted] •Synthesis of pyrazolo[3,4-d]pyrimidines derivatives endowed with nM Ki values.•Best compound exerted good cytotoxicity activity against…”
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Si113-prodrugs selectively activated by plasmin against hepatocellular and ovarian carcinoma
Published in European journal of medicinal chemistry (05-11-2021)“…Si113, a pyrazolo[3,4-d]pyrimidine derivative, gained more attention as an anticancer agent due to its potent anticancer activity on both in vitro and in vivo…”
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Abstract 2201: Preclinical development of novel pyrazolo[3,4- d ]pyrimidines structure-based TKIs for the treatment of glioblastoma
Published in Cancer research (Chicago, Ill.) (01-07-2019)“…Abstract The aim of this study was the preclinical development of a set of pyrazolo[3,4-d]pyrimidine structure-based small molecules ATP-competitive SRC…”
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Prodrugs of Pyrazolo[3,4‑d]pyrimidines: From Library Synthesis to Evaluation as Potential Anticancer Agents in an Orthotopic Glioblastoma Model
Published in Journal of medicinal chemistry (27-07-2017)“…Pyrazolo[3,4-d]pyrimidines are potent protein kinase inhibitors with promising antitumor activity but suboptimal aqueous solubility, consequently worth being…”
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Identification of new pyrrolo[2,3-d]pyrimidines as Src tyrosine kinase inhibitors in vitro active against Glioblastoma
Published in European journal of medicinal chemistry (15-02-2017)“…In the last few years, several pyrrolo-pyrimidine derivatives have been either approved by the US FDA and in other countries for the treatment of different…”
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Pyrazolo[3,4-d]pyrimidines-loaded human serum albumin (HSA) nanoparticles: Preparation, characterization and cytotoxicity evaluation against neuroblastoma cell line
Published in Bioorganic & medicinal chemistry letters (15-07-2017)“…[Display omitted] Pyrazolo[3,4-d]pyrimidine derivatives 1–5, active as c-Src inhibitors, have been selected to be formulated as drug-loaded human serum albumin…”
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Synthesis and biological evaluation of a library of hybrid derivatives as inhibitors of influenza virus PA-PB1 interaction
Published in European journal of medicinal chemistry (05-09-2018)“…The limited treatment options against influenza virus along with the growing public health concerns regarding the continuous emergence of drug-resistant…”
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High-throughput docking for the identification of new influenza A virus polymerase inhibitors targeting the PA-PB1 protein-protein interaction
Published in Bioorganic & medicinal chemistry letters (01-01-2014)“…A high-throughput molecular docking approach was successfully applied for the selection of potential inhibitors of the Influenza RNA-polymerase which act by…”
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4,6-Diphenylpyridines as Promising Novel Anti-Influenza Agents Targeting the PA–PB1 Protein–Protein Interaction: Structure–Activity Relationships Exploration with the Aid of Molecular Modeling
Published in Journal of medicinal chemistry (24-03-2016)“…Influenza is an infectious disease that represents an important public health burden, with high impact on the global morbidity, mortality, and economy. The…”
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Combining X‑ray Crystallography and Molecular Modeling toward the Optimization of Pyrazolo[3,4‑d]pyrimidines as Potent c‑Src Inhibitors Active in Vivo against Neuroblastoma
Published in Journal of medicinal chemistry (08-01-2015)“…c-Src is a tyrosine kinase belonging to the Src-family kinases. It is overexpressed and/or hyperactivated in a variety of cancer cells, thus its inhibition has…”
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Protein–protein interactions and human cellular cofactors as new targets for HIV therapy
Published in Current opinion in pharmacology (01-10-2014)“…Highlights • Insight into new strategies in HIV therapy. • Targeting protein–protein interactions in HIV. • Targeting cellular cofactors in HIV…”
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Identification of a new family of pyrazolo[3,4-d]pyrimidine derivatives as multitarget Fyn-Blk-Lyn inhibitors active on B- and T-lymphoma cell lines
Published in European journal of medicinal chemistry (01-11-2019)“…Abnormal activation of B-cell receptor (BCR) signaling plays a key role in the development of lymphoid malignancies, and could be reverted by the simultaneous…”
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Insight into the Allosteric Inhibition of Abl Kinase
Published in Journal of chemical information and modeling (27-05-2014)“…Abl kinase inhibitors targeting the ATP binding pocket are currently used as a front-line therapy for the treatment of chronic myelogenous leukemia (CML), but…”
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Pyrrolo[2,3-d]pyrimidines active as Btk inhibitors
Published in Expert opinion on therapeutic patents (02-12-2017)“…Btk is a tyrosine kinase dysregulated in several B-cell malignancies and autoimmune diseases, and this has given rise to a search for Btk inhibitors…”
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A New Strategy for Glioblastoma Treatment: In Vitro and In Vivo Preclinical Characterization of Si306, a Pyrazolo[3,4- d ]Pyrimidine Dual Src/P-Glycoprotein Inhibitor
Published in Cancers (19-06-2019)“…Overexpression of P-glycoprotein (P-gp) and other ATP-binding cassette (ABC) transporters in multidrug resistant (MDR) cancer cells is responsible for the…”
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