Based on our previous work, a novel class of 8-cyclopentyl-7,8-dihydropteridin-6(5H)-one derivatives were synthesized and evaluated as antiproliferative agents. Structure-activity relationship analysis revealed that the greatest activities were achieved with a 4-(4-methylpiperazin-1-yl)aniline group at C-2 position of dihydropteridin-6(5H)-one core, and the most promising compound 6k demonstrated comparable antiproliferative activity with Palbociclib and more potent than our parent derivative 4 toward four cell lines including HCT-116, HeLa, HT-29, and MDA-MB-231 with IC values of 3.29, 6.75, 7.56, and 10.30 μM, respectively. Moreover, the mechanism studies revealed that compound 6k could induce cell cycle arrest at G2/M phase via a concentration-dependent manner. In general, these preliminary observations suggested that these compounds could serve as promising scaffolds for further modification to develop novel and highly potent cancer therapy agents.
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http://dx.doi.org/10.1016/j.bmcl.2020.127684 | DOI Listing |
Ecotoxicol Environ Saf
January 2025
Department of Stomatology, the Affiliated Suzhou Hospital of Nanjing Medical University, Suzhou Municipal Hospital, Gusu School, Nanjing Medical University, No. 242, Guangji Road, Suzhou, Jiangsu Province 215000, China. Electronic address:
Exposure to 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) in utero can result in osteogenic defect during palatogenesis, but the effects on other craniofacial bones and underlying mechanisms remain to be characterized. By treating pregnant mice with TCDD (40 μg/kg) at the vital craniofacial patterning stages (embryonic day 8.5, 10.
View Article and Find Full Text PDFJ Breath Res
January 2025
School of Medicine and Pharmacy, Ocean University of China, 5 Yushan Rd, Qingdao, Shandong, 266003, CHINA.
Lung cancer is one of the most common malignancy in the world, and early detection of lung cancer remains a challenge. The exhaled breath condensate (EBC) from lung and trachea can be collected totally noninvasively. In this study, our aim is to identify differential metabolites between non-small cell lung cancer (NSCLC) and control EBC samples and discriminate NSCLC group from control group by orthogonal projections to latent structures-discriminant analysis (OPLS-DA) models.
View Article and Find Full Text PDFACS Appl Mater Interfaces
January 2025
Konkuk University, 120 Neungdong-ro, Gwangjin-gu, Seoul 05029, Republic of Korea.
Organic solar cells (OSCs) have recently achieved efficiencies of >20% in single-junction unit cells owing to rapid advancements in materials and device technologies. Large-area OSCs face several challenges that adversely affect their efficiency compared to small unit cells. These challenges include increased resistance loads derived from their larger dimensions, as well as limitations related to morphology, miscibility, and crystallinity.
View Article and Find Full Text PDFACS Appl Bio Mater
January 2025
Institute of Physics and Materials Science, Department of Natural Sciences and Sustainable Ressources, BOKU University, Peter Jordan-Straß 82, 1190 Vienna, Austria.
Spider silk (SPSI) is a promising candidate for use as a filler material in nerve guidance conduits (NGCs), facilitating peripheral nerve regeneration by providing a scaffold for Schwann cells (SCs) and axonal growth. However, the specific properties of SPSI that contribute to its regenerative success remain unclear. In this study, the egg sac silk of is investigated, which contains two distinct fiber types: tubuliform (TU) and major ampullate (MA) silk.
View Article and Find Full Text PDFAdv Sci (Weinh)
January 2025
Department of Orthopaedics, The First Affiliated Hospital of Soochow University, Orthopedic Institute, MOE Key Laboratory of Geriatric Diseases and Immunology, Suzhou Medical College, Soochow University, Suzhou, Jiangsu, 215000, China.
Extracellular matrix (ECM) derived from mesenchymal stem cells regulates antioxidant properties and bone metabolism by providing a favorable extracellular microenvironment. However, its functional role and molecular mechanism in mitochondrial function regulation and aged bone regeneration remain insufficiently elucidated. This proteomic analysis has revealed a greater abundance of proteins supporting mitochondrial function in the young ECM (Y-ECM) secreted by young bone marrow-derived mesenchymal stem cells (BMMSCs) compared to the aged ECM (A-ECM).
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