Results 271 to 280 of about 354,000 (376)

A Cytotoxic Indazole‐based Gold(III) Carboxamide Pincer Complex Targeting DNA Through Dual Binding Modes of Groove Binding and Alkylation

open access: yesChemistry – A European Journal, EarlyView.
Toward new gold(III) anticancer agents. Herein, we report on an indazole‐based gold(III) carboxamide pincer complex exhibiting significant cytotoxicity, likely mediated through dual interactions with DNA. Mechanistic investigations suggest that the complex binds to the DNA and forms specific interactions with nucleotide bases.
Rufaro Razuwika   +4 more
wiley   +1 more source

The use of strong analgesics for prehospital pain management in children in the region of Southern Denmark: a register-based study. [PDF]

open access: yesScand J Trauma Resusc Emerg Med
Colding-Jørgensen JT   +9 more
europepmc   +1 more source

Exploring Tyramine's Role in the Formation of Supramolecular Adducts with Nonsteroidal Anti‐Inflammatory Drugs

open access: yesChemistry – A European Journal, EarlyView.
An a priori design approach identified tyramine as an ideal co‐former for obtaining new supramolecular adducts with nonsteroidal anti‐inflammatory drugs, speeding up the co‐crystallization process. Three novel adducts and a new polymorphic form were synthesized and thoroughly characterized by solid‐state NMR and single‐crystal XRD.
Chiara Rosso   +6 more
wiley   +1 more source

Isoniazid‐Dihydropyrimidinone Molecular Hybrids: Design, Synthesis, Antitubercular Activity, and Cytotoxicity Investigations with Computational Validation

open access: yesChemMedChem, EarlyView.
Antitubercular evaluation of a novel library of isoniazid‐dihydropyrimidinone molecular hybrids (8a–8n) discloses a potent compound with MIC = 0.39μg mL−1 against M. tuberculosis mc26230. Cytotoxicity, stability, and in silico studies, including molecular docking and ADME/T (absorption, distribution, metabolism, excretion, and toxicity) analysis ...
Gobind Kumar   +10 more
wiley   +1 more source

Further SAR of GIRK1/2 activators: Synthesis and Biological Characterization of In Vitro Tool Compounds

open access: yesChemMedChem, Accepted Article.
The work presented herein outlines the ongoing structure‐activity relationship (SAR) studies centered around a potent, efficacious, and selective activators of the GIRK1/2 channel. Optimization studies centered around the pyrazole privileged scaffold, the N‐1‐position of the pyrazole and the right‐hand ether.
Sumaiya Nahid   +8 more
wiley   +1 more source

A Randomized Phase 1 Study Evaluating Pharmacokinetics, Safety, and Tolerability of a High‐Concentration, Long‐Acting Cabotegravir Formulation in Adults Without HIV

open access: yesClinical Pharmacology in Drug Development, EarlyView.
Abstract Long‐acting (LA) cabotegravir 200‐mg/mL (CAB200) injections are approved for HIV‐1 prevention and as a complete LA HIV‐1 treatment regimen with rilpivirine. A high‐concentration suspension formulation, cabotegravir 400 mg/mL (CAB400‐D), was developed to enable less frequent dosing and self‐administration. This phase 1, double‐blind, randomized
Kelong Han   +16 more
wiley   +1 more source

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