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Identification of a 7H-pyrrolo[2,3-d]pyrimidin derivatives as selective type II c-Met/Axl inhibitors with potent antitumor efficacy.
Bioorg Chem
January 2025
Center for Preclinical Safety Evaluation of Drugs, State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, China. Electronic address:
In this study, we reported the discovery of a novel type II c-Met/Axl inhibitor, characterized by using 4-amino-7H-pyrrolo[2,3-d]pyrimidine as a hinge region binder. Through a systematic exploration of the structure-activity relationship, based on the clinically reported c-Met inhibitor BMS-777607, we identified the optimized compound 22a. 22a exhibited remarkable potency against c-Met and Axl kinases, with IC values of 1 nM and 10 nM, respectively, and demonstrated over 100-fold selectivity to other members of the TAM subfamily.
View Article and Find Full Text PDFNovel Approaches to Monitor Pharmacokinetics and Metabolism of Gemcitabine-Ibandronate Conjugate in Mice and Dogs.
Molecules
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 PDFEnergy Metabolism and Stemness and the Role of Lauric Acid in Reversing 5-Fluorouracil Resistance in Colorectal Cancer Cells.
Int J Mol Sci
January 2025
Department of Molecular Pathology, Nara Medical University School of Medicine, Kashihara 634-8521, Japan.
While 5-fluorouracil (5FU) plays a central role in chemotherapy for colorectal cancer (CRC), resistance to 5FU remains a major challenge in CRC treatment, and its underlying mechanisms remain unclear. In this study, we investigated the relationship between 5FU resistance acquisition, stemness, and energy metabolism. Among the two CRC cell lines, HT29 cells exhibited glycolytic and quiescent properties, while CT26 cells relied on oxidative phosphorylation (OXPHOS) for energy.
View Article and Find Full Text PDF[Efficient synthesis of polydatin by a two-enzyme coupled with one-pot method].
Sheng Wu Gong Cheng Xue Bao
January 2025
School of Biological and Pharmaceutical Engineering, West Anhui University, Lu'an 237012, Anhui, China.
Traditional Chinese medicine of has been utilized in China for thousands of years. Its primary active compound, polydatin, exhibits a variety of pharmacological effects including the regulation of glucose and lipid metabolism, suppression of cough and asthma, as well as antibacterial and anti-inflammatory properties. However, conventional methods for polydatin production are inadequate to satisfy the market demand.
View Article and Find Full Text PDFSynthesis, molecular dynamics simulation and antimicrobial activity of novel s-triazine clubbed with three different hybrid pharmacophores.
Biochem Biophys Res Commun
January 2025
Molecular Biophysics and Structural Biology (MBSB) Group, Department of Biochemistry, University of Johannesburg, Auckland Park Kingsway Campus, 2006, South Africa. Electronic address:
To address microbial infections and combat drug resistance, we designed, synthesized, and evaluated three novel s-triazine clubbed pharmacophores: 1-acetylpyrazoline (5a-e), 2-aminopyrimidine (6a-e), and 1,5-benzodiazepine (7a-e). These were derived from chalcone (4a-e), showing improved pharmacological profiles. The compounds underwent characterization by FTIR, NMR, and Mass Spectroscopy, and their antimicrobial activities, along with structure-activity relationships (SAR), were assessed using in silico and in vitro methods.
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