Voreloxin (SNS-595) is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.

AuM1Phe, an N-heterocyclic carbene (NHC) metal complex, inhibits both human topoisomerase I activity and actin polymerization. It also impedes the proliferation of MDA-MB-231 breast cancer cells, exhibiting an IC50 value of 1.2 μM [1].

1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV/AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.

Topoisomerase IV inhibitor 2 (compound 7d) is a potent inhibitor of DNA topoisomerase IV (TOPO IV), exhibiting IC50 values of 0.23 μM for TOPO IV and 0.43 μM for DNA gyrase. It also demonstrates antibacterial efficacy, with minimum inhibitory concentrations (MICs) of 0.972 μM against Staphylococcus aureus Newman and 0.608 μM against Escherichia coli ATCC8739 [1].

Topoisomerase IV inhibitor 2 (compound 5d) is a potent inhibitor of DNA topoisomerase IV (TOPO IV), exhibiting IC50 values of 0.35 μM for TOPO IV and 0.55 μM for DNA gyrase. It also demonstrates antibacterial properties, with minimum inhibitory concentrations (MICs) of 1.985 μM against Staphylococcus aureus Newman and 0.744 μM against Escherichia coli ATCC8739 [1].