Novel multimetallic copper pyrazolate complexes, inaccessible using simple pyrazole ligands due to competing, alternative structural motifs, can be obtained by locking pairs of pyrazole ligands together with ethylene tethers. Nanojars based on this tethered pyrazole ligand display unexpected total selectivity for the carbonate over the sulfate ion.
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http://dx.doi.org/10.1039/c6cc09197k | DOI Listing |
Bioorg Chem
January 2025
Department of Chemistry, Faculty of Science, Al-Azhar University, Cairo 11754 Egypt.
The vascular endothelial growth factor receptor is essential for the angiogenesis of cancer. Tumor propagation was effectively suppressed by inhibiting VEGFR-2 activity. As a result, the target quinoxaline-pyrazole hybrids were created in a way that closely resembled the structural characteristics of VEGFR-2 inhibitors.
View Article and Find Full Text PDFCancer Med
January 2025
Department of Urology, Keio University School of Medicine, Tokyo, Japan.
Introduction: Avelumab, an anti-programmed death ligand 1 antibody, was approved in combination with axitinib for curatively unresectable or metastatic renal cell carcinoma (RCC) in Japan in December 2019. Because the pivotal JAVELIN Renal 101 study included a limited number of Japanese patients, post-marketing surveillance (PMS) was required to evaluate outcomes (safety and effectiveness) in patients with RCC who received avelumab + axitinib treatment in clinical practice in Japan.
Materials And Methods: We report data from prospective, noncomparative, multicenter, observational PMS in patients with RCC who received ≥ 1 dose of avelumab.
ACS Omega
January 2025
Department of Chemistry-BMC Biochemistry, University of Uppsala, Husargatan 3, Uppsala 75237, Sweden.
In this work, we present the synthesis, solid-state characterization, and studies of two pyrazole derivatives: 5-(2-methylphenoxy)-3-methyl-1-phenyl-1-pyrazole-4-carbaldehyde (I) and 5-(4-methylphenoxy)-3-methyl-1-phenyl-1-pyrazole-4-carbaldehyde (II). The molecular crystal properties, in terms of intermolecular hydrogen bonds and other weak interactions, are analyzed using single crystal X-ray diffraction. The Hirshfeld surfaces computational method is used to quantify the intermolecular interactions, density functional theory for theoretical structural optimization, and its comparison with the experimental structure and studies using docking and molecular dynamics studies of I and II with CDC7-kinase.
View Article and Find Full Text PDFComput Biol Chem
January 2025
Drug Discovery and Development Laboratory (DDD Lab), Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India. Electronic address:
Multiple myeloma (MM) is the second most frequently diagnosed hematological malignancy, presenting limited treatment options with no curative potential and significant drug resistance. Recent studies involving genetic knockdown established the crucial role of GRK6 in upholding the viability of MM cells, emphasizing the need to identify potential inhibitors. Computational exploration of GRK6 inhibitors has not been attempted previously.
View Article and Find Full Text PDFDalton Trans
January 2025
School of Chemistry, The University of New South Wales (UNSW), Kensington, Sydney, 2052, Australia.
The synthesis and structural characterisation of [Ln(Tp)]I (1-Ln; Ln = La, Ce, Pr, Nd) (Tp = hydrotris(3-(2'-furyl)-pyrazol-1-yl)borate) have been reported as an isomorphous series adopting pseudo-icosahedral ligand field geometries. Continuous shape measurement (CShM) analyses on the crystal field environments of 1-Ln show the smallest values yet reported for complexes employing two hexadentate ligands (-scorpionate environments), with the smallest belonging to 1-La. Single-ion magnetism for 1-Ce, 1-Pr and 1-Nd was probed with ac magnetic susceptibility studies revealing slow magnetic relaxation for 1-Nd in applied magnetic fields and in zero-applied field for 1-Ce, which is a rare observation for Ce(III)-based single-ion magnets.
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