Cyclometallated π-allyliridium C,O-benzoates modified with (S)-tol-BINAP, which are stable to air, water, and SiO , catalyze highly enantioselective N-allylations of indoles and related azoles. This reaction complements previously reported metal-catalyzed indole allylations in that complete levels of N versus C3 and branched versus linear regioselectivity are observed.
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http://dx.doi.org/10.1002/anie.201902799 | DOI Listing |
Cell Mol Biol (Noisy-le-grand)
January 2025
Department of Pharmacology, Faculty of Pharmacy, Mersin University, Mersin, Türkiye.
Increasing evidence suggests that inhibition of receptor-interacting serine/threonine-protein kinase (RIPK) 1/RIPK3/mixed lineage kinase domain-like pseudokinase (MLKL) necrosome has protective effects in vivo models of painful conditions seen in humans associated with inflammation and demyelination in the central nervous system. However, the contribution of RIPK1-driven necroptosis to inflammatory pain remains unknown. Therefore, this study aims to determine the effect of necrostatin (Nec) -1s, a selective RIPK1 inhibitor, on lipopolysaccharide (LPS)-induced inflammatory pain and related underlying mechanisms.
View Article and Find Full Text PDFChem Biol Drug Des
January 2025
Department of Molecular Biology and Biochemistry, University of California, Irvine, California, USA.
A new series of 13 ritonavir-like inhibitors of human drug-metabolizing CYP3A4 was rationally designed to study the R side-group and R end-group interplay when the R side-group is represented by phenyl. Spectral, functional, and structural characterization showed no improvement in the binding affinity and inhibitory potency of R/R-phenyl inhibitors upon elongation and/or fluorination of R-Boc (tert-butyloxycarbonyl) or its replacement with benzenesulfonyl. When R is pyridine, the impact of R-phenyl-to-indole/naphthalene substitution was multidirectional and highly dependent on side-group stereo configuration.
View Article and Find Full Text PDFVet Med Sci
January 2025
Department of Surgery, Faculty of Veterinary Medicine, Atatürk University, Erzurum, Turkey.
Objectives: Vomiting is frequently observed in cats after dexmedetomidine administration. This study aimed to compare the efficacy of different antiemetics in preventing vomiting in cats after dexmedetomidine administration.
Methods: Sixty-four cats were randomly allocated to receive saline solution (0.
Int J Biol Sci
January 2025
Department of Urology, the Fourth Affiliated Hospital of School of Medicine, and International School of Medicine, International Institutes of Medicine, Zhejiang University, Yiwu, China.
Clear cell renal cell carcinoma (ccRCC) is one of the most common and aggressive malignancies of the urinary system. Despite being the first-line treatment for advanced ccRCC, vascular endothelial growth factor receptor inhibitors (VEGFRis) face significant limitations due to both initial and acquired resistance, which impede complete tumor eradication. Using a CRISPR/Cas9 library screening approach, was identified as a resistance-associated gene for three prevalent VEGFRis (Sunitinib, Axitinib, and Sorafenib).
View Article and Find Full Text PDFCan Vet J
January 2025
Department of Small Animal Clinical Sciences (Cormillot, Weissman, MacDonald-Dickinson) and Department of Veterinary Pathology (Dickinson), Western College of Veterinary MeDicine, University of Saskatchewan, 52 Campus Drive, Saskatoon, Saskatchewan S7N 5B4.
A 16-year-old castrated male domestic medium-hair cat was referred for examination of multiple cutaneous mast cell tumors displaying epitheliotropism. Staging tests were negative for distant metastasis. Toceranib phosphate therapy was initiated.
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