Results 61 to 70 of about 991,719 (279)

Cryptotanshinone attenuates LPS-induced acute lung injury by regulating metabolic reprogramming of macrophage

open access: yesFrontiers in Medicine, 2023
BackgroundAcute lung injury (ALI) is a life-threatening inflammatory disease without effective therapeutic regimen. Macrophage polarization plays a key role in the initiation and resolution of pulmonary inflammation.
Zesen Ye   +7 more
doaj   +1 more source

Enantioselective Access to Trifluoromethylated Spirocyclopropyl Heterocycles

open access: yesAdvanced Science, EarlyView.
We report a rhodium‐catalyzed asymmetric [2+1] spirocyclopropanation of methylene azacycles with trifluoromethyl carbenes in situ derived from fluoroalkyl triftosylhydrazones. ABSTRACT Chiral spirocyclopropyl heterocycles have emerged as privileged three‐dimensional structural motifs in medicinal chemistry.
Yuanhao Zhu   +9 more
wiley   +1 more source

Pharmacokinetics-Driven Evaluation of the Antioxidant Activity of Curcuminoids and Their Major Reduced Metabolites—A Medicinal Chemistry Approach

open access: yesMolecules, 2021
Curcuminoids are the main bioactive components of the well-known Asian spice and traditional medicine turmeric. Curcuminoids have poor chemical stability and bioavailability; in vivo they are rapidly metabolized to a set of bioreduced derivatives and/or ...
Gábor Girst   +4 more
doaj   +1 more source

Correction to Impact of Lipophilic Efficiency on Compound Quality

open access: yes, 2016
Correction to Impact of Lipophilic Efficiency on Compound ...
György M. Keserű (1269681)   +2 more
core   +1 more source

Pigmented Rice Bioactive Compound Possible Mechanism from Breast Cancer.

open access: yes, 2023
Pigmented Rice Bioactive Compound Possible Mechanism from Breast Cancer.
Alexander Patera Nugraha (9084650)
core   +1 more source

AS‐TLC‐Based High‐Throughput Screening Integrated with CuAAC Optimization Strategy Facilitates the Rapid Discovery of YTHDC1 Inhibitor

open access: yesAdvanced Science, EarlyView.
We developed Affinity Selection Thin‐Layer Chromatography (AS‐TLC) as a method for high‐throughput screening (HTS) of compound mixtures. Furthermore, we integrated activity assays with AS‐TLC and identified a YTH domain‐containing protein 1 (YTHDC1) inhibitor. Building on this hit, we applied copper(I)‐catalyzed azide–alkyne cycloaddition (CuAAC) click
Mingchen Wang   +19 more
wiley   +1 more source

Tocopherol and Tocotrienol Content in the Leaves of the Genus Hypericum: Impact of Species and Drying Technique

open access: yesPlants
α-Tocopherol (α-T) predominates in photosynthetic tissues, while tocotrienols (T3s) are reported very rarely. The genus Hypericum stands out as one of the few exceptions.
Ieva Miķelsone   +3 more
doaj   +1 more source

Exploring the mode of action of bioactive compounds by microfluidic transcriptional profiling in mycobacteria. [PDF]

open access: yes, 2013
Most candidate anti-bacterials are identified on the basis of their whole cell anti-bacterial activity. A critical bottleneck in the early discovery of novel anti-bacterials is tracking the structure activity relationship (SAR) of the novel compounds ...
Thomas Dick   +60 more
core   +2 more sources

Mesenchymal Stromal Cell‐Based Cell–Drug Conjugates for the Treatment of Acute Liver Failure

open access: yesAdvanced Science, EarlyView.
Mesenchymal stromal cell (MSC)‐based cell‐drug conjugates are constructed by anchoring rosiglitazone‐loaded nanoparticles onto the MSC surface. Sustained rosiglitazone release enhances MSC proliferation and paracrine activity while promoting anti‐inflammatory macrophage polarization.
Tenghui Ye   +6 more
wiley   +1 more source

Beyond Nature's Blueprint: Macrocyclic Peptides Containing Unnatural Amino Acids in Therapeutic Development

open access: yesAngewandte Chemie, EarlyView.
Strategic incorporation of unnatural amino acids transforms macrocyclic peptides into drug‐like molecules capable of engaging challenging targets. These building blocks enhance stability, permeability, and bioavailability, accelerating the development of next‐generation peptide therapeutics.
Krishna K. Sharma   +5 more
wiley   +2 more sources

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