In this report, we synthesized some pyrimidine derivatives by multi-component reaction of urea, benzaldehydes, and 1,3-indandione in the presence of ZIF-8/ZnFeO/GO-OSOH nanocomposite under reflux conditions. Initially, graphene oxide was prepared from graphite, and then it was sulfonated using ClOSOH. Next, GO-OSOH nanosheets were used to support ZIF-8/ZnFeO nanostructure. The construction of the synthesized structure was established using different spectral techniques such as X-ray crystallography (XRD), scanning electron microscopy (SEM), energy dispersive X-ray spectroscopy (EDX/Mapping), Fourier transform infrared (FTIR), thermal gravimetric analysis (TGA), vibrating sample magnetometer (VSM), and Brunauer-Emmett-Teller (BET). The present method provides various benefits including the efficiency of outcomes, easy separation of the catalyst, and excellent yield of the products within short reaction times. Moreover, the antibacterial activities of pyrimidine derivatives were investigated via the agar-well diffusion method on gram-negative () and gram-positive () bacteria and the obtained results illustrated reasonable effects.
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http://dx.doi.org/10.1016/j.heliyon.2024.e26339 | DOI Listing |
Nat Commun
January 2025
Division of Molecular Genetics, German Cancer Research Center (DKFZ), Heidelberg, Germany.
Chronic lymphocytic leukemia is a malignant lymphoproliferative disorder for which primary or acquired drug resistance represents a major challenge. To investigate the underlying molecular mechanisms, we generate a mouse model of ibrutinib resistance, in which, after initial treatment response, relapse under therapy occurrs with an aggressive outgrowth of malignant cells, resembling observations in patients. A comparative analysis of exome, transcriptome and proteome of sorted leukemic murine cells during treatment and after relapse suggests alterations in the proteasome activity as a driver of ibrutinib resistance.
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January 2025
Research Institute of Pharmaceutical Sciences, College of Pharmacy, Kyungpook National University, 80 Daehak-ro, Buk-gu, Daegu 702-701, Republic of Korea.
A thiazolo-pyrimidinone derivative library was developed through a facile solid-phase synthesis method. For the reaction, the thiazolo[4,5-]pyrimidin-7(6)-one structure was synthesized through efficient Thorpe-Ziegler and cyclization reactions. The thiazolo[4,5-]pyrimidin-7(6)-one derivative library with a diversity of three had a total of four synthesis steps and 57 compounds.
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January 2025
Chair and Department of Biochemistry and Pharmacogenomics, Medical University of Warsaw, 1 Banacha Str., 02-097 Warsaw, Poland.
Vitamin B (thiamine) plays an important role in human metabolism. It is essential for the proper growth and development of the body and has a positive effect on the functioning of the digestive, cardiovascular, and nervous systems. Additionally, it stimulates the brain and improves the psycho-emotional state.
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January 2025
MBC Pharma Inc., Aurora, CO 80045, USA.
Background: The use of the bone-seeking properties of bisphosphonates (BPs) to target the delivery of therapeutic drugs is a promising approach for the treatment of bone metastases. Currently, the most advanced example of this approach is a gemcitabine-ibandronate conjugate (GEM-IB), where the bone-targeting BP ibandronate (IB) is covalently linked to the antineoplastic agent gemcitabine (GEM) via a spacer phosphate group. In the present study, we describe the development of a new analytical platform to evaluate the metabolism and pharmacokinetics of GEM-IB in mice and dogs and the results of proof-of-concept studies assessing the pharmacokinetics of GEM-IB in dogs and mice.
View Article and Find Full Text PDFInt J Mol Sci
January 2025
Department of Medical Biophysics, Institute of Biophysics, Faculty of Biology and Environmental Protection, University of Lodz, 90-236 Lodz, Poland.
Hepatocellular carcinoma (HCC) cells critically depend on PARP1 and CHK1 activation for survival. Combining the PARP inhibitor (PARPi) olaparib with a CHK1 inhibitor (MK-8776, CHK1i) produced a synergistic effect, reducing cell viability and inducing marked oxidative stress and DNA damage, particularly in the HepG2 cells. This dual treatment significantly increased apoptosis markers, including γH2AX and caspase-3/7 activity.
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