Search Results - "Roman, Bart I"
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Glioblastoma-Associated Mesenchymal Stem/Stromal Cells and Cancer-Associated Fibroblasts: Partners in Crime?
Published in International journal of molecular sciences (01-02-2024)“…Tumor-associated mesenchymal stem/stromal cells (TA-MSCs) have been recognized as attractive therapeutic targets in several cancer types, due to their ability…”
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Vehicle development, pharmacokinetics and toxicity of the anti-invasive agent 4-fluoro-3',4',5'-trimethoxychalcone in rodents
Published in PloS one (22-02-2018)“…Effective inhibitors of invasion and metastasis represent a serious unmet clinical need. We have recently identified 4-fluoro-3',4',5'-trimethoxychalcone or…”
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3
Transglucosylation potential of six sucrose phosphorylases toward different classes of acceptors
Published in Carbohydrate research (27-09-2011)“…In this study, the transglucosylation potential of six sucrose phosphorylase (SP) enzymes has been compared using eighty putative acceptors from different…”
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The Expanding Role of Chemistry in Optimizing Proteins for Human Health Applications: Miniperspective
Published in Journal of medicinal chemistry (10-06-2021)“…Over the past decades, therapeutics based on biological macromolecules and cells have successfully entered the clinical arena and progressively occupied an…”
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The Expanding Role of Chemistry in Optimizing Proteins for Human Health Applications
Published in Journal of medicinal chemistry (10-06-2021)“…Over the past decades, therapeutics based on biological macromolecules and cells have successfully entered the clinical arena and progressively occupied an…”
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6
Design, synthesis and structure–activity relationships of some novel, highly potent anti-invasive (E)- and (Z)-stilbenes
Published in Bioorganic & medicinal chemistry (01-09-2013)“…In our ongoing exploration of the structure–activity landscape of anti-invasive chalcones, we have prepared and evaluated a number of structurally related (E)-…”
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Medicinal Chemistry and Use of Myosin II Inhibitor (S)‑Blebbistatin and Its Derivatives
Published in Journal of medicinal chemistry (08-11-2018)“…(S)-Blebbistatin, a chiral tetrahydropyrroloquinolinone, is a widely used and well-characterized ATPase inhibitor selective for myosin II. The central role of…”
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8
Recovering Actives in Multi-Antitarget and Target Design of Analogs of the Myosin II Inhibitor Blebbistatin
Published in Frontiers in chemistry (24-05-2018)“…In multitarget drug design, it is critical to identify active and inactive compounds against a variety of targets and antitargets. Multitarget strategies thus…”
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Microbial inhibition of oral epithelial wound recovery: potential role for quorum sensing molecules?
Published in AMB Express (21-05-2015)“…Awareness of the impact of microbiota in both health and disease is growing. Using a new in vitro oral mucosa co-culture model, we recently showed a clear…”
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Synthesis of isoindoles and related iso-condensed heteroaromatic pyrroles
Published in Chemical Society reviews (07-09-2012)“…Over the past few years, isoindoles have found wide application in materials science. Isoindole containing BODIPY dyes are highly fluorescent materials and…”
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11
Homogeneous Gold-Catalyzed Cyclization Reactions of Alkynes with N- and S-Nucleophiles
Published in Advanced synthesis & catalysis (12-10-2015)“…This review covers the formation of N‐ and S‐containing heterocycles, initiated by gold‐catalyzed nucleophilic attack of N‐ or S‐nucleophiles onto alkynes…”
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12
Essay: Avoiding unfounded health claims on small molecules in scientific literature
Published in Bioorganic chemistry (01-05-2019)“…[Display omitted] •Unfounded health claims pollute scientific literature.•Discussion of human and scientific causes.•Suggestion of corrective actions to be…”
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Improved synthesis and comparative analysis of the tool properties of new and existing D-ring modified (S)-blebbistatin analogs
Published in European journal of medicinal chemistry (18-08-2017)“…(S)-Blebbistatin is a widely used research tool to study myosin II, an important regulator of many motility based diseases. Its potency is too low to be of…”
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Insights into the myosin II inhibitory potency of A-ring-modified (S)-blebbistatin analogs
Published in Bioorganic & medicinal chemistry letters (01-07-2017)“…[Display omitted] Myosin II is an interesting target for therapeutic intervention, as it is involved in a large number of motility-based diseases…”
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Synthesis and Biological Activity of Oxazolopyrimidines
Published in European journal of organic chemistry (24-05-2018)“…In this work, the synthesis of oxazolo[4,5‐d]pyrimidines and oxazolo[5,4‐d]pyrimidines is reviewed. The review is focused on the construction of the scaffold…”
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Synthesis of C-ring-modified blebbistatin derivatives and evaluation of their myosin II ATPase inhibitory potency
Published in Bioorganic & medicinal chemistry letters (15-07-2018)“…[Display omitted] •First report on C-ring-modified blebbistatin analogs.•Incorporation of hydroxymethyl or allyloxymethyl functionalities.•Additional favorable…”
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Discovery of (S)-3'-hydroxyblebbistatin and (S)-3'-aminoblebbistatin: polar myosin II inhibitors with superior research tool properties
Published in Organic & biomolecular chemistry (01-03-2017)“…In search of myosin II inhibitors with superior research tool properties, a chemical optimization campaign of the blebbistatin scaffold was conducted in this…”
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Continuous‐Flow Synthesis of Phenothiazine Antipsychotics: A Feasibility Study
Published in European journal of organic chemistry (14-02-2019)“…The continuous flow synthesis of a model phenothiazine antipsychotic is presented herein, using 3‐chloropropionyl chloride as a central building block. The…”
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Atom‐ and Mass‐economical Continuous Flow Production of 3‐Chloropropionyl Chloride and its Subsequent Amidation
Published in Chemistry : a European journal (09-08-2018)“…3‐Chloropropionyl chloride is a chemically versatile building block with applications in the field of adhesives, pharmaceuticals, herbicides and fungicides…”
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Synthesis of β-, γ-, δ-, ..., ω-Halogenated Ketones and Aldehydes
Published in Chemical reviews (13-10-2010)Get full text
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