ChemMedChem
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Prodrug Strategies in Anticancer ChemotherapyAbstract The majority of clinically approved anticancer drugs are characterized by a narrow therapeutic window that results mainly from a high systemic toxicity of the drugs in combination with an evident lack of tumor selectivity. Besides the development of suitable galenic formulations such as liposomes or micelles, several promising prodrug approaches have been f... ...
ChemMedChem - Tập 3 Số 1 - Trang 20-53 - 2008
Modelling Inhalational Anaesthetics Using Bayesian Feature Selection and QSAR Modelling MethodsAbstract The development of robust and predictive QSAR models is highly dependent on the use of molecular descriptors that contain information relevant to the property being modelled. Selection of these relevant features from a large pool of possibilities is difficult to achieve effectively. Modern Bayesian methods provide substantial advantages over co...
ChemMedChem - Tập 5 Số 8 - Trang 1318-1323 - 2010
Isoxazolines: A Novel Chemotype Highly Effective on EctoparasitesAbstract Efficient control of arthropod ectoparasite infestations has a long‐standing history in the agriculture and veterinary sectors, aiming to decrease the parasite burden of affected crops and animals. Ligand‐gated chloride channels (LGCCs) modulated by γ‐aminobutyric acid (GABA) and glutamate have been identified as suitable molecular targets, and several clas... ...
ChemMedChem - Tập 11 Số 3 - Trang 270-276 - 2016
Transthyretin Mimetics as Anti‐β‐Amyloid Agents: A Comparison of Peptide and Protein ApproachesAbstract β‐Amyloid (Aβ) aggregation is causally linked to neuronal pathology in Alzheimer's disease; therefore, several small molecules, antibodies, and peptides have been tested as anti‐Aβ agents. We developed two compounds based on the Aβ‐binding domain of transthyretin (TTR): a cyclic peptide cG8 and an engineered protein mTTR, and compared them for therapeutical... ...
ChemMedChem - Tập 13 Số 9 - Trang 968-979 - 2018
SHOP: A Method For Structure‐Based Fragment and Scaffold HoppingAbstract We present a method for fragment/scaffold substitution based on protein–ligand interactions. This concept goes beyond bioisosteric replacement, which only uses the structure of the fragment to replace as query. The methodology is validated with more than 10 biological targets relevant for drug discovery. hiện toàn bộ
ChemMedChem - Tập 4 Số 3 - Trang 427-439 - 2009
Pharmacophore‐Based Discovery of Small‐Molecule Inhibitors of Protein–Protein Interactions between HIV‐1 Integrase and Cellular Cofactor LEDGF/p75Abstract The cellular protein lens epithelium‐derived growth factor, or transcriptional coactivator p75 (LEDGF/p75), plays a crucial role in HIV integration. The protein–protein interactions (PPIs) between HIV‐1 integrase (IN) and its cellular cofactor LEDGF/p75 may therefore serve as targets for the development of new anti‐HIV drugs. In this work, a st...
ChemMedChem - Tập 4 Số 8 - Trang 1311-1316 - 2009
Curcumin‐Derived Pyrazoles and Isoxazoles: Swiss Army Knives or Blunt Tools for Alzheimer's Disease?Abstract Curcumin binds to the amyloid β peptide (Aβ) and inhibits or modulates amyloid precursor protein (APP) metabolism. Therefore, curcumin‐derived isoxazoles and pyrazoles were synthesized to minimize the metal chelation properties of curcumin. The decreased rotational freedom and absence of stereoisomers was predicted to enhance affinity toward Aβ42<... ...
ChemMedChem - Tập 3 Số 1 - Trang 165-172 - 2008
Synthesis of a Heparan Sulfate Mimetic Library Targeting FGF and VEGF via Click Chemistry on a Monosaccharide TemplateAbstract A disulfated methyl 6‐azido‐6‐deoxy‐α‐D ‐mannopyranoside template was used as a core structure for binding to the angiogenic growth factors FGF‐1, FGF‐2, and VEGF. The core structure was diversified in a rapid, parallel manner by employing the CuI ‐catalyzed Huisgen azide–alkyne cycloaddition (“click”) reaction. The div... ...
ChemMedChem - Tập 7 Số 7 - Trang 1267-1275 - 2012
Development of an (S)‐1‐{2‐[Tris(4‐methoxyphenyl)methoxy]ethyl}piperidine‐3‐carboxylic acid [(S)‐SNAP‐5114] Carba Analogue Inhibitor for Murine γ‐Aminobutyric Acid Transporter Type 4Abstract A series of GABA uptake inhibitors related to (S )‐1‐{2‐[tris(4‐methoxyphenyl)methoxy]ethyl}piperidine‐3‐carboxylic acid [(S )‐SNAP‐5114], the most potent mGAT4 inhibitor known so far, were synthesized and biologically evaluated for their inhibitory potency at the four GABA uptake transporters mGAT1–4 stab... ...
ChemMedChem - Tập 7 Số 7 - Trang 1245-1255 - 2012
Design, Synthesis, and Biological Evaluation of Levoglucosenone‐Derived Ras Activation InhibitorsAbstract A panel of new potential Ras ligands was generated by decorating a tricyclic levoglucosenone‐derived scaffold with aromatic moieties. Some members of the panel show in vitro inhibitory activity toward the nucleotide exchange process on Ras and are toxic to some human cancer cell lines.
ChemMedChem - Tập 4 Số 4 - Trang 524-528 - 2009
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