Stefania Baraldi
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View article: Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2-<i>d</i>]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors
Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2-<i>d</i>]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors Open
The clinical evidence for the success of tyrosine kinase inhibitors in combination with microtubule-targeting agents prompted us to design and develop single agents that possess both epidermal growth factor receptor (EGFR) kinase and tubul…
View article: Cover Image, Volume 38, Issue 4
Cover Image, Volume 38, Issue 4 Open
On the cover: The cover image, by Kenneth A. Jacobson et al., is based on the Review Article A3 Adenosine Receptors as Modulators of Inflammation: From Medicinal Chemistry to Therapy, https://doi.org/10.1002/med.21456.
View article: Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors
Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors Open
Monoacylglycerol lipase (MAGL) is a serine hydrolase that plays an important role in the degradation of the endocannabinoid neurotransmitter 2-arachidonoylglycerol, which is implicated in many physiological processes. Beyond the possible u…
View article: A2A Adenosine Receptor: Structures, Modeling, and Medicinal Chemistry
A2A Adenosine Receptor: Structures, Modeling, and Medicinal Chemistry Open
Many selective agonists and antagonists of the A 2A adenosine receptor (AR) have been reported, while allosteric modulators specific for this receptor are still needed. Many heterocyclic chemotypes have been discovered as A 2A AR antagonis…
View article: Synthesis and biological evaluation of alpha-bromoacryloylamido indolyl pyridinyl propenones as potent apoptotic inducers in human leukaemia cells
Synthesis and biological evaluation of alpha-bromoacryloylamido indolyl pyridinyl propenones as potent apoptotic inducers in human leukaemia cells Open
The combination of two pharmacophores into a single molecule represents one of the methods that can be adopted for the synthesis of new anticancer molecules. To investigate the influence of the position of the pyridine nitrogen on biologic…
View article: A<sub>3</sub>Adenosine Receptors as Modulators of Inflammation: From Medicinal Chemistry to Therapy
A<sub>3</sub>Adenosine Receptors as Modulators of Inflammation: From Medicinal Chemistry to Therapy Open
The A 3 adenosine receptor (A 3 AR) subtype is a novel, promising therapeutic target for inflammatory diseases, such as rheumatoid arthritis (RA) and psoriasis, as well as liver cancer. A 3 AR is coupled to inhibition of adenylyl cyclase a…
View article: Medicinal Chemistry, Pharmacology, and Clinical Implications of TRPV1 Receptor Antagonists
Medicinal Chemistry, Pharmacology, and Clinical Implications of TRPV1 Receptor Antagonists Open
Transient receptor potential vanilloid 1 (TRPV1) is an ion channel expressed on sensory neurons triggering an influx of cations. TRPV1 receptors function as homotetramers responsive to heat, proinflammatory substances, lipoxygenase product…
View article: Design and Synthesis of Potent in Vitro and in Vivo Anticancer Agents Based on 1-(3′,4′,5′-Trimethoxyphenyl)-2-Aryl-1H-Imidazole
Design and Synthesis of Potent in Vitro and in Vivo Anticancer Agents Based on 1-(3′,4′,5′-Trimethoxyphenyl)-2-Aryl-1H-Imidazole Open
A novel series of tubulin polymerization inhibitors, based on the 1-(3′,4′,5′-trimethoxyphenyl)-2-aryl-1 H -imidazole scaffold and designed as cis -restricted combretastatin A-4 analogues, was synthesized with the goal of evaluating the ef…
View article: One-Pot Reaction To Obtain N,N′-Disubstituted Guanidines of Pyrazolo[4,3-<i>e</i>][1,2,4]triazolo[1,5-<i>c</i>]pyrimidine Scaffold as Human A<sub>3</sub>Adenosine Receptor Antagonists
One-Pot Reaction To Obtain N,N′-Disubstituted Guanidines of Pyrazolo[4,3-<i>e</i>][1,2,4]triazolo[1,5-<i>c</i>]pyrimidine Scaffold as Human A<sub>3</sub>Adenosine Receptor Antagonists Open
In this paper we describe an extension SAR study of pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine nucleus as A3AR antagonist. Our initial aim was to replace the phenylcarbamoyl moiety at the 5 position of PTP nucleus with a thiourea func…
View article: Design, Synthesis, and Biological Evaluation of Novel 2-((2-(4-(Substituted)phenylpiperazin-1-yl)ethyl)amino)-5′-<i>N</i>-ethylcarboxamidoadenosines as Potent and Selective Agonists of the A<sub>2A</sub>Adenosine Receptor
Design, Synthesis, and Biological Evaluation of Novel 2-((2-(4-(Substituted)phenylpiperazin-1-yl)ethyl)amino)-5′-<i>N</i>-ethylcarboxamidoadenosines as Potent and Selective Agonists of the A<sub>2A</sub>Adenosine Receptor Open
Stimulation of A2A adenosine receptors (AR) promotes anti-inflammatory responses in animal models of allergic rhinitis, asthma, chronic obstructive pulmonary disease, and rheumatic diseases. Herein we describe the results of a research pro…