WebbTopoisomerase I Inhibitors and Anti-cancer Agents Khac-Minh Thai *, Quang-Huynh Bui, Thanh-Dao Tran and Thi-Ngoc-Phuong Huynh Department of Medicinal Chemistry, School of Pharmacy, University of Medicine and Pharmacy at Ho Chi Minh City, 41 Dinh Tien Hoang St., Dist. 1, Ho Chi Minh City, Vietnam; Webb17 apr. 2024 · In this article, we will introduce an anti-cancer agent Pirarubicin. Pirarubicin is an anthracycline antibiotic and also a potent inhibitor of Topoisomerase II . Pirarubicin is a topoisomerase II inhibitor. This compound shows inhibitory activities against M5076 and Ehrlich cells, with IC50s of 0.366 and 0.078 μM, respectively.
Benzimidazoles: Selective Inhibitors of Topoisomerase I with ...
WebbTopoisomerase Inhibitor Selectively Replicating Oncolytic Adenoviruses Combined with Chemotherapy, Radiotherapy, or Molecular Targeted Therapy... Neoplasia. Stan K. … Webb19 feb. 2024 · In this study, a drug discovery programme that sought to identify novel dual bacterial topoisomerase II inhibitors (NBTIs) led to the selection of six optimized compounds. In enzymatic assays, the molecules showed equivalent dual-targeting activity against the DNA gyrase and topoisomerase IV enzymes of Staphylococcus aureus … bring out your rubbish day hull
Identification of Naphthoquinones Derivatives as Inhibitors of …
WebbInhibitors of the topoisomerase enzymes stop DNA replication, RNA transcription, and repair of DNA damage. The complex between DNA and topoisomerase II is normally temporary, quickly dissolving. The inhibitor drugs can stabilize the complex, ending the mitotic processes. WebbFurthermore, the study suggests that the hydrazono-quinoline analogs exert their antibacterial activity as dual inhibitors for DNA gyrase and DNA topoisomerase IV enzymes with IC 50 values ranging between (4.56 ± 0.3 - 21.67 ± 0.45) and (6.77 ± 0.4 - 20.41 ± 0.32) μM, respectively. WebbThe Topo I inhibitors used in clinical practice are mostly water-soluble derivatives of camptothecin, and the Topo II inhibitors with better effect are podophyllotoxin derivatives, such as etoposide. The structure and activity of topoisomerase targeting agents are shown in Table 1. Mechanism of Topoisomerases bring out your game