Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
a series of 6-substituted dihydrobenzophenanthridine alkaloids were synthesized by introduction of different functional groups to C-6 of dihydrobenzophenanthridine backbone. The preliminary anti-inflammatory activities of all compounds were screened by investigating the inhibitory ability on NO production in LPS-stimulated RAW 264.7 cells. Among synthesized compounds, 6-(N-phenyl)-aminocarbonyl methyl dihydrochelerythrine (compound 12b) showed increased anti-inflammatory ability and decreased cytotoxicity and could inhibit the expression of pro-inflammatory factors TNF-α and IL-6 in RAW 264.7 macrophages. The anti-inflammatory ability of compound 12b was further evaluated using DSS-induced mice colitis models based on colonic tissue damage assessment, histopathological assessment and immunohistochemical analysis. In vivoexperiment revealed that compound 12b had good alleviating effect on acute colitis in mice. In conclusion, compound 12b may be a promising anti-inflammatory lead compound.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmc.2025.118145 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Design, synthesis and biological evaluation of triazolo[1,5-a]pyrimidine derivatives as new antiproliferative agents with multikinase inhibitory activity.
Bioorg Chem
August 2025
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ain Shams University, P.O. Box 11566, Abbassia, Cairo, Egypt. Electronic address:
Two series of triazolo[1,5-a]pyrimidines were designed and synthesized as antiproliferative agents targeting multi kinase inhibition aiming to increase potency and combat drug resistance. The synthesized compounds were tested for their antiproliferative activity. The triazolopyrimidine derivatives 9b, 9c, 12b and 12c showed promising anticancer activities, in particular, compounds 12b and 12c displayed broad spectrum antiproliferative potential against NCI cancer cell lines with GI mean value of 10.
View Article and Find Full Text PDFStructure-based design of alicyclic fused pyrazole derivatives for targeting TGF-β receptor I kinase: molecular docking and dynamics insights.
J Comput Aided Mol Des
September 2025
Supramolecular and Catalysis Lab, Department of Natural Products Chemistry, School of Chemistry, Madurai Kamaraj University, Madurai, Tamil Nadu, India.
TGF-β receptor I kinase plays a significant role in cancer biology and is a well-established target for cancer drug development, as evidenced by active molecules like Galunisertib (LY2157229). Computational studies were conducted to analyse the catalytic site of TGF-β receptor I kinase, identifying key amino acid residues essential for binding. Based on these findings, Alicyclic fused pyrazole derivatives were designed.
View Article and Find Full Text PDFA Convenient, Pd-Free Approach to the Synthesis of Risdiplam.
Molecules
August 2025
Medicinal Biotechnology Department, Sirius University of Science and Technology, Olimpiyskiy Ave. 1, 354340 Sirius, Krasnodar Region, Russia.
Several approaches to the synthesis of risdiplam, a pharmacologically relevant pyridopyrimidinone derivative, have been recently reported. However, most of these routes rely exclusively on palladium-catalyzed, cross-coupling reactions and involve low-yielding intermediates, which limit their scalability and complicate impurity control. In this work, we present a five-step, straightforward route to risdiplam, utilizing ethyl 2,8-dimethylimidazo[1,2-]pyridazine-3-carboxylate-an accessible and cost-effective building block previously developed by our research group-as a starting material.
View Article and Find Full Text PDFA medium-bandgap acceptor incorporating a novel electron-rich building block enables efficient organic photovoltaics.
J Colloid Interface Sci
August 2025
Department of Chemistry, University of Science and Technology of China, Hefei 230026, China; Key Laboratory of Functional Molecular Solids, Ministry of Education, Anhui Laboratory of Molecule-Based Materials and School of Chemistry and Materials Science, Anhui Normal University, Wuhu 241002, China.
Organic photovoltaics (OPVs) have emerged as a highly promising renewable energy technology due to their solution-processability, mechanical flexibility, and potential for low-cost manufacturing. Despite remarkable progress, further improving the power conversion efficiencies (PCEs) remains a critical challenge for their commercial applications. The incorporation of medium-bandgap non-fullerene acceptors (NFAs) as third components in ternary OPV devices has proven particularly effective in enhancing device performance.
View Article and Find Full Text PDFDesign, synthesis and anti-influenza A virus activity of N-containing heterocyclic glycyrrhetinic acid derivatives.
Bioorg Med Chem Lett
August 2025
Department of Pharmacy, PLA Naval Medical Center, Naval Medical University, Shanghai 200052, China. Electronic address:
Glycyrrhetinic acid (GA), a bioactive triterpenoid derived from Glycyrrhiza glabra, exhibits broad-spectrum antiviral properties but suffers from poor solubility and bioavailability. To enhance its anti-influenza activity, we designed and synthesized 12 novel nitrogen-containing heterocyclic GA derivatives through structural modifications at the A-ring (C-2/C-3) and C-30 position. All compounds were evaluated against influenza A/H1N1 virus in 293T cells.
View Article and Find Full Text PDF