Several sulfonamides having pyrrole (5a-c, 8, 11b-19, 23, 24), pyrrolo[2,3-d] pyrimidine (6, 7, 10, 20, 21, 25) and pyrrolo[2,3-b]pyridine (22) were synthesized and evaluated for their antitumor and radioprotective activities. The structure of the synthesized compounds was elucidated by elemental analyses and spectral data. Compounds 5a, 16, 17, 19, and 23 displayed more potent antitumor activities than the reference drug, doxorubicin. On the other hand compounds 19, 23 and 25 exhibited radioprotective activities.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1055/s-0031-1296742 | DOI Listing |
J Control Release
January 2025
College of Pharmaceutical Sciences, College of Chemistry, Chemical Engineering and Materials Science,, Soochow University, Suzhou 215123, People's Republic of China; State Key Laboratory of Radiation Medicine and Protection, Soochow University, Suzhou 215123, People's Republic of China. Electronic address:
Vaccination may cure cancer patients by inducing tumor-specific immune responses. Radiotherapy is an appealing strategy to generate cancer vaccines in situ; thus far, however, only modest and short-lived immune responses are achieved. We here show that radiation combined with co-activating STING-TLR9 can generate powerful in situ cancer vaccines.
View Article and Find Full Text PDFRadiat Oncol J
December 2024
Radiation Oncology Unit, 1st Department of Radiology, Medical School, Aretaieion Hospital, National and Kapodistrian University of Athens, Athens, Greece.
Purpose: Neoadjuvant radiotherapy (RT) or chemoradiotherapy (CRT) is the standard treatment for locally advanced rectal adenocarcinoma. The recent emerging data on preoperative immunotherapy as an effective therapeutic modality for mismatch repair deficient rectal carcinomas suggests that the immune system plays a significant role in tumor eradication. Although RT has been shown to stimulate anti-tumor immunity, it also leads to substantial lymphopenia, hindering the effect of immune response.
View Article and Find Full Text PDFEur J Med Chem
February 2025
Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guizhou Medical University, Guiyang, 550004, China. Electronic address:
FMS-like tyrosine receptor kinase 3 (FLT3) mutations, the most common genetic alterations found in acute myeloid leukemia (AML) patients, have been pursued as an ideal drug discovery target for the AML therapy. Taking compound 2 as lead, a series of pyridine derivatives bearing 1,2,3-triazole moiety were rationally designed and synthesized. The bioassays confirmed that these derivatives exerted potent antileukemia effects, and compound 12y was found to be the most potent one.
View Article and Find Full Text PDFBiomaterials
May 2025
Center for Molecular Imaging and Nuclear Medicine, State Key Laboratory of Radiation Medicine and Protection, School of Radiation Medicine and Protection, Collaborative Innovation Center of Radiological Medicine of Jiangsu Higher Education Institutions, Soochow University, Suzhou 215123, China. Electronic address:
The cross-talk between lysosomes and mitochondria is crucial for keeping intracellular homeostasis and metabolic function, providing a promising approach for tumor therapy. Herein, we employed polyvinylpyrrolidone (PVP)-modified Cu-gallic acid (CuGA) complex nano-boosters for amplifying lysosomes-mitochondria cascaded damage, and thereby effectively inducing cuproptosis and pyroptosis of breast tumor cells to boost anti-tumor immunotherapy. The CuGA nano-boosters could hijack lysosomal iron to form a bimetallic catalyst Cu(Fe)GA in situ through ion-exchange reaction, and cause the release of Cu and metal ion dysregulation (i.
View Article and Find Full Text PDFBiomaterials
May 2025
State Key Laboratory of Radiation Medicine and Protection, School of Radiation Medicine and Protection & School for Radiological and Interdisciplinary Sciences (RAD-X), Collaborative Innovation Center of Radiation Medicine of Jiangsu Higher Education Institutions, Soochow University, Suzhou 215123, China. Electronic address:
Radiotherapy (RT) can trigger immunogenic cell death (ICD) in tumor cells and release adenosine triphosphate (ATP) to activate antitumor immunity. However, the formation of immunosuppressive adenosine (ADO) mediated by ectonucleotidases including CD39 and CD73, can exacerbate the immunosuppressive effects. Herein, a radiosensitizer-based metal-organic framework (MOF) composed of bismuth (Bi) and ellagic acid (EA) was synthesized in situ on the surface of Escherichia coli Nissle 1917 (EcN) to serve as a carrier for the CD39 inhibitor sodium polyoxotungstate (POM-1).
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!