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Discovery of novel thienopyridine indole derivatives as inhibitors of tubulin polymerization targeting the colchicine-binding site with potent anticancer activities.
Eur J Med Chem
January 2025
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou, 450001, China. Electronic address:
Based on the molecular hybridization strategy, novel thienopyridine indole derivatives were designed and synthesized as tubulin polymerization inhibitors, and the in vitro antiproliferative potency on MGC-803, KYSE450 and HCT-116 cells was evaluated. Among them, compound 20b showed a broad-spectrum antiproliferative activity against 11 cancer cell lines, with IC values below 4 nmol/L. Notably, it demonstrated exceptional efficacy against MGC-803 (IC = 1.
View Article and Find Full Text PDFHypoxia-Targeted-Therapy: Mussel-inspired hollow polydopamine nanocarrier containing MoS nanozyme and tirapazamine with anti-angiogenesis property for synergistic tumor therapy.
J Colloid Interface Sci
January 2025
Department of Chemical Engineering, National Taiwan University of Science and Technology, Taipei 106335 Taiwan. Electronic address:
Photothermal therapy (PTT) using thermal and tumor microenvironment-responsive reagents is promising for cancer treatment. This study demonstrates an effective PTT nanodrug consisting of hollow-structured, thermally sensitive polydopamine nanobowls (HPDA NB), molybdenum sulfide (MoS) nanozyme, and tirapazamine (TPZ; a hypoxia-responsive drug), with a structure of HPDA@TPZ/MoS NBs which is hereafter denoted as HPTZMoS NBs. With the Fenton-like activity, the HPTZMoS NBs in the presence of HO catalyze the formation of hydroxyl radicals, providing chemodynamic therapy (CDT) effect and deactivating glutathione.
View Article and Find Full Text PDFDual-drug loaded chondroitin sulfate embolization beads enhance TACE therapy for HCC by integrating embolization, chemotherapy, and anti-angiogenesis.
Mater Today Bio
February 2025
State Key Laboratory of Digital Medical Engineering, Jiangsu Key Laboratory for Biomaterials and Devices, School of Biological Sciences & Medical Engineering, Southeast University, Nanjing, 210009, China.
Hepatocellular carcinoma (HCC) is a major public health threat due to its high incidence and mortality rates. Transcatheter arterial chemoembolization (TACE), the primary treatment for intermediate-to-advanced hepatocellular carcinoma (HCC), commonly utilizes embolic agents loaded with anthracycline-based cytotoxic drugs. Post-TACE, the hypoxic microenvironment in the tumor induced by embolization stimulates the formation of new blood vessels, potentially leading to revascularization and diminishing TACE's efficacy.
View Article and Find Full Text PDFA cRGD-modified liposome for targeted delivery of artesunate to inhibit angiogenesis in endometriosis.
Biomater Sci
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Department of Gynecology, The Sixth Affiliated Hospital, Sun Yat-Sen University, Guangzhou, Guangdong 510655, China.
Currently, hormonal therapy for endometriosis faces challenges in achieving a balance between treatment and preserving the chance of pregnancy. Therefore, the development of non-hormonal therapy holds significant clinical importance. Angiogenesis is a hallmark of endometriosis, and anti-angiogenic therapies targeting the hypoxia-inducible factor-1α (HIF-1α) pathway are considered potential approaches for endometriosis.
View Article and Find Full Text PDFThe Suppression of Signal Transducer and Activator of Transcription-3 in A549 human Lung Carcinoma Cells Induced by Marine Sponge .
J Exp Pharmacol
January 2025
Department of Pharmacology and Clinical Pharmacy, Faculty of Pharmacy, Universitas Padjadjaran, Jatinangor, Indonesia.
Introduction: Lung cancer is recognized as a highly lethal disease, demanding swift and accurate solutions. Previous analysis showed the cytotoxic impact of extract containing ergost-22-en-3-one and ergost-7-en3-ol against A549 lung cancer cells, with an IC value of 9.38 μg/mL.
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