Novel Fluoroindenoisoquinoline Non-Camptothecin Topoisomerase I Inhibitors [PDF]
Molecular Cancer Therapeutics, 2018 Abstract Contrary to other anticancer targets, topoisomerase I (TOP1) is targeted by only one chemical class of FDA-approved drugs: topotecan and irinotecan, the derivatives of the plant alkaloid, camptothecin. The indenoisoquinolines LMP400, LMP744, and LMP776 are novel noncamptothecin TOP1 inhibitors in clinical trial, which ...
Laetitia Marzi +10 more
openaire +3 more sources
Enhanced Stability and Bioactivity of Natural Anticancer Topoisomerase I Inhibitors through Cyclodextrin Complexation [PDF]
Pharmaceutics, 2021 The use of cyclodextrins as drug nano-carrier systems for drug delivery is gaining importance in the pharmaceutical industry due to the interesting pharmacokinetic properties of the resulting inclusion complexes.
Víctor González-Ruiz +9 more
doaj +2 more sources
Dual-acting histone deacetylase-topoisomerase I inhibitors [PDF]
Bioorganic & Medicinal Chemistry Letters, 2013 Current chemotherapy regimens are comprised mostly of single-target drugs which are often plagued by toxic side effects and resistance development. A pharmacological strategy for circumventing these drawbacks could involve designing multivalent ligands that can modulate multiple targets while avoiding the toxicity of a single-targeted agent.
William, Guerrant +5 more
openaire +3 more sources
Discovery of DNA Topoisomerase I Inhibitors with Low-Cytotoxicity Based on Virtual Screening from Natural Products [PDF]
Marine Drugs, 2017 Currently, DNA topoisomerase I (Topo I) inhibitors constitute a family of antitumor agents with demonstrated clinical effects on human malignancies. However, the clinical uses of these agents have been greatly limited due to their severe toxic effects ...
Lan-Ting Xin +10 more
doaj +2 more sources
Phosphine Oxide Indenoquinoline Derivatives: Synthesis and Biological Evaluation as Topoisomerase I Inhibitors and Antiproliferative Agents [PDF]
MoleculesThe synthesis of phosphorous indenoquinolines and their biological evaluation as topoisomerase 1 (TOP1) inhibitors and antiproliferative agents were performed.
Alba Rodriguez-Paniagua +4 more
doaj +2 more sources
Small DNA circles as bacterial topoisomerase I inhibitors [PDF]
RSC Advances, 2019 It is demonstrated that small DNA circles showed high inhibitory effect on the activity of bacterial topoisomerase I and the single-stranded regions associated with bending deformation are believed to be the crucial factor for trapping the enzymes.
Dawei Li +4 more
openaire +4 more sources
Tumor-targeted top1 inhibitor delivery with optimized parp inhibition in advanced solid tumors: a phase i trial of gapped scheduling [PDF]
Nature CommunicationsDespite mechanistic rationale for combining PARP inhibitors with topoisomerase I inhibitors, clinical use has been hindered by dose-limiting toxicities.
Anish Thomas +12 more
doaj +2 more sources
Encapsulation and Enhanced Delivery of Topoisomerase I Inhibitors in Functionalized Carbon Nanotubes [PDF]
ACS Omega, 2018 Sieun Chae +10 more
doaj +2 more sources
Communications Biology, 2023 Two potent inhibitors PPEF and BPVF of bacterial TopoIA enzymes function by impairing DNA binding and thus DNA cleavage and relaxation activities of bacterial topoisomerase I enzymes.
Vikas Maurya +9 more
doaj +1 more source
Thoracic Cancer, 2022 Background Small cell lung cancer (SCLC) is a highly aggressive disease with a poor prognosis. Although most patients initially respond to topoisomerase inhibitors, resistance rapidly emerges.
Miwako Omori +8 more
doaj +1 more source