We previously reported that several 7-alkoxy-4-phenylamino-3-quinolinecarbonitriles were potent inhibitors of Src kinase activity. We disclose here a new highly efficient and versatile route to these compounds, which are also potent inhibitors of Abl kinase.
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http://dx.doi.org/10.1021/jm0499458 | DOI Listing |
Bioorg Chem
January 2025
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Istanbul University 34116 Istanbul, Turkey.
In this study, new 2-indolinone-indole hybrid compounds (4a-s) carrying a benzoyl moiety were synthesized and their cytotoxic effects were examined against pancreatic (MIA-PaCa-2) and colon (HT-29 and HCT-116) cancer cells by MTT assays. Most of the tested compounds exhibited a better inhibitory activity and safety profile than the reference standard sunitinib malate against MIA-PaCa-2 and HCT-116 cancer cells. Compound 4e displayed the greatest cytotoxic effect on HCT-116 cell with an IC value of 0.
View Article and Find Full Text PDFBioorg Chem
January 2025
Department of In Vitro Carcinogenesis and Cellular Chemotherapy, Chittaranjan National Cancer Institute, 37, S. P. Mukherjee Road, Kolkata 700026, India. Electronic address:
Histone deacetylases (HDACs) play a critical role in chromatin remodelling and modulating the activity of various histone proteins. Aberrant HDAC functions has been related to the progression of breast cancer (BC), making HDAC inhibitors (HDACi) promising small-molecule therapeutics for its treatment. Hydroxamic acid (HA) is a significant pharmacophore due to its strong metal-chelating ability, HDAC inhibition properties, MMP inhibition abilities, and more.
View Article and Find Full Text PDFInt Immunopharmacol
January 2025
Department of Orthopedics, The Second Hospital of Jilin University, Changchun 130041, China.
Corynoline (COR) is an isoquinoline alkaloid derived from the traditional Chinese medicine Corydalis bungeana Turcz, known for its analgesic, antibacterial, neuroprotective, and osteoporosis-alleviating properties. However, its potential molecular effects against osteosarcoma (OS) remain unclear, warranting further investigation. This study demonstrated that COR inhibits OS cell proliferation and promotes apoptosis in a dose-dependent manner.
View Article and Find Full Text PDFTzu Chi Med J
September 2024
School of Medicine, Tzu Chi University, Hualien, Taiwan.
Objectives: Gastric cancer (GC) is one of the most malignant tumors. Mounting studies highlighted gastric cancer stem cells (GCSCs) were responsible for the failure of treatment due to recurrence and drug resistance of advanced GC. However, targeted therapy against GCSC for improving GC prognosis suffered from lack of suitable models and molecular targets in terms of personalized medicine.
View Article and Find Full Text PDFFront Pharmacol
January 2025
Department of Emergency Intensive Care Unit, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan, China.
Introduction: In patients with acute respiratory distress syndrome, mechanical ventilation often leads to ventilation-induced lung injury (VILI), which is attributed to unphysiological lung strain (UPLS) in respiratory dynamics. Platelet endothelial cell adhesion molecule-1 (PECAM-1), a transmembrane receptor, senses mechanical signals. The Src/STAT3 pathway plays a crucial role in the mechanotransduction network, concurrently triggering pyroptosis related inflammatory responses.
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