A new hybrid template was designed by combining the structural features of phosphodiesterase 4 (PDE4) inhibitors with several heterocyclic moieties which present an integral part in the skeleton of many apoptotic agents. Thirteen compounds of the synthesized hybrids displayed higher inhibitory activity against PDE4B than the reference drug, roflumilast. Further investigation indicated that compounds 13b and 20 arrested the cell cycle at the G2/M phase and the pre-G1 phase, and induced cell death by apoptosis of A549 cells in a caspase-dependent manner.
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http://dx.doi.org/10.1002/ardp.201700403 | DOI Listing |
Assay Drug Dev Technol
January 2025
University Institute of Pharmacy, Pandit Ravishankar Shukla University, Raipur, India.
Ther Adv Respir Dis
January 2025
University of Texas Health San Antonio and the South Texas Veterans Health Care System, San Antonio, TX, USA.
Idiopathic pulmonary fibrosis (IPF) is often regarded as the archetypal progressive fibrosing interstitial lung disease (ILD). The term "progressive pulmonary fibrosis" (PPF) generally describes progressive lung fibrosis in an individual with an ILD other than IPF. Both IPF and PPF are associated with loss of lung function, worsening dyspnea and quality of life, and premature death.
View Article and Find Full Text PDFEur J Pharmacol
February 2025
The School of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, Guangzhou, 510006, PR China. Electronic address:
Glioblastoma multiforme (GBM) is a highly heterogeneous and aggressive brain tumor, which presents significant challenges for treatment in clinical settings. Phosphodiesterase 4 (PDE4) inhibitors can prevent the degradation of cAMP and have been used as a potential targeted therapeutic approach for different cancer types. However, their clinical use is restricted by side effects such as nausea and vomiting.
View Article and Find Full Text PDFFront Immunol
December 2024
Department of Experimental Medicine, University of Rome "Tor Vergata", Rome, Italy.
Introduction: Fungi, including , may be a trigger or exacerbate psoriasis, especially in difficult to treat (DTT) areas, through the activation of IL-17/23 axis.
Methods: In this study, seventy patients with DDT psoriasis were enrolled to evaluate species and/or other opportunistic fungi colonization rate at baseline (T0) and the impact of apremilast on fungal load, clinical outcome, serum cytokine levels and biochemical serum profile of patients after 16, 24 and 52 weeks of treatment.
Results: In our population, 33 (47%) patients were colonized by spp.
RMD Open
December 2024
David Geffen School of Medicine, University of California Los Angeles, Los Angeles, California, USA.
Interstitial lung disease (ILD) associated with rheumatoid arthritis or with connective tissue diseases such as systemic sclerosis can be collectively named systemic autoimmune rheumatic disease-associated ILDs (SARD-ILDs) or rheumatic musculoskeletal disorder-associated ILDs. SARD-ILDs result in substantial morbidity and mortality, and there is a high medical need for effective therapies that target both fibrotic and inflammatory pathways in SARD-ILD. Phosphodiesterase 4 (PDE4) hydrolyses cyclic AMP, which regulates multiple pathways involved in inflammatory processes.
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