A novel series of malonamide-type dual VEGFR2/c-Met inhibitors in which one of the amide bonds was replaced by an amide isostere-a trifluoroethylamine unit, was designed, synthesized, and evaluated for their enzymatic and cellular inhibition of VEGFR2 and c-Met enzymes. Optimization of these molecular entities resulted in identification of potent and selective inhibitors of VEGFR2 enzyme.
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http://dx.doi.org/10.1016/j.bmcl.2009.12.099 | DOI Listing |
Front Parasitol
April 2024
Institut für Parasitologie, Biomedizinisches Forschungszentrum Seltersberg (BFS), Justus Liebig Universitaet Giessen, Giessen, Germany.
Introduction: Schistosomiasis has for many years relied on a single drug, praziquantel (PZQ) for treatment of the disease. Immense efforts have been invested in the discovery of protein kinase (PK) inhibitors; however, given that the majority of PKs are still not targeted by an inhibitor with a useful level of selectivity, there is a compelling need to expand the chemical space available for synthesizing new, potent, and selective PK inhibitors. Small-molecule inhibitors targeting the ATP pocket of the catalytic domain of PKs have the potential to become drugs devoid of (major) side effects, particularly if they bind selectively.
View Article and Find Full Text PDFTheranostics
January 2025
State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, Nankai University, Tianjin 300353, People's Republic of China.
Hepatic carcinoma, one of the most malignant cancers in the world, has limited success with immunotherapy and a poor prognosis in patients. While pyroptosis is considered as a promising immunotherapy strategy for tumors, it still suffers from a lack of effective inducers. We designed, synthesized and screened an indole analogue, , featuring a 2, 4-thiazolidinedione substituted indole scaffold.
View Article and Find Full Text PDFNPJ Sci Food
January 2025
Department of Pharmacognosy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.
This study compared two Annona squamosa L. cultivars, Abdelrazik (Annona A.) and Balady (Annona B.
View Article and Find Full Text PDFSci Prog
January 2025
Department of Food Science and Technology, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana.
Objective: This study investigated the fungal contamination profile of cocoa beans from cocoa-growing regions in Ghana, with particular emphasis on the potential impact of ochratoxigenic species.
Methods: A total of 104 fermented and dried cocoa beans were randomly collected from farmers for analysis. Fungal isolation was conducted using potato dextrose agar and malt extract agar media.
Comput Biol Chem
January 2025
School of Computational and Integrative Sciences, Jawaharlal Nehru University, New Delhi 110067, India. Electronic address:
Drug resistance poses a major obstacle to the efficient treatment of colorectal cancer (CRC), which is one of the cancers that kill people most often in the United States. Advanced colorectal cancer patients frequently pass away from the illness, even with advancements in chemotherapy and targeted therapies. Developing new biomarkers and therapeutic targets is essential to enhancing prognosis and therapy effectiveness.
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