topoisomerase inhibitor 5

Topoisomerase inhibitor 5 (compound 158) is an inhibitor of bacterial topoisomerase, with a minimum inhibitory concentration of 0.125 μg/mL, and exhibits anti-tuberculosis activity.

Topoisomerase I inhibitor 5 is an efficient topoisomerase I inhibitor with an IC50 value, effectively disrupting DNA and inhibiting topoisomerase I activity. It induces apoptosis in MCF-7 cells and arrests the cell cycle at the G1 phase, displaying potency in reversing P-gp-mediated resistance to Adriamycin [1].

Topoisomerase II inhibitor 5 (Compound E24) is a DNA topoisomerase II inhibitor with anticancer properties.

TopoisomeraseI/II inhibitor 5 (compound 1) stabilizes G4 structures through binding and concurrently inhibits the relaxation activities of TopoI and II.

AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50= 0.36 nM).1AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.2,3AZD 1152 inhibits tumor xenograft growthin vivo.4,5 1.Mortlock, A.A., Foote, K.M., Heron, N.M., et al.Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinaseJ. Med. Chem.50(9)2213-2224(2007) 2.Popescu, R., Heiss, E.H., Ferk, F., et al.Ikarugamycin induces DNA damage, intracellular calcium increase, p38 MAP kinase activation and apoptosis in HL-60 human promyelocytic leukemia cellsMutation Research709-71060-66(2011) 3.Moore, A.S., Blagg, J., Linardopoulos, S., et al.Aurora kinase inhibitors: Novel small molecules with promising activity in acute myeloid and Philadelphia-positive leukemiasLeukemia24(4)671-678(2010) 4.Wilkinson, R.W., Odedra, R., Heaton, S.P., et al.AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosisClin. Cancer. Res13(12)3682-3688(2007) 5.Yang, J., Ikezoe, T., Nishioka, C., et al.AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivoBlood110(6)2034-2040(2007)

TAS-103 is a dual inhibitor of DNA topoisomerase I/II, utilized in cancer research.

Intoplicine (RP 60475) dimesylate is a DNA topoisomerase I and II inhibitor belonging to the 7H-benzo[e]pyrido[4,3-b]indole series. It exhibits a strong affinity for DNA (K A = 2 x 10^5 /M), resulting in increased linear DNA length.

Topoisomerase II inhibitor 6 (Compound 5), a tryptanthrin derivative, is a potent and selective topoisomerase II inhibitor that blocks the CCRF-CEM cell cycle in the G2 phase and induces DNA double-strand breaks (DSB). It exhibits antiproliferative activity on various tumor cell lines and has potential for cancer research [1].

Topoisomerase IIα-IN-2 (compound 5) is a potent inhibitor of the topoisomerase TopoIIα and a DNA-binding ligand. It exhibits high anti-proliferative activity in human cancer cell lines, arrests the cell cycle in the G2/M phase, and significantly induces DNA damage.

NBTIs-IN-5 (Compound 5r) is a novel bacterial topoisomerase inhibitor (NBTI) DNA gyrase inhibitor that acts on Mycobacterium abscessus (Mabs) DNA procyclase (IC50: 1.5 μM), showing inhibitory effects on the growth of Mabsbamboo bacteria (MIC90: 0.4 μM).

Daunorubicin (Daunomycin) citrate, a potent anti-tumor anthracycline antibiotic, acts as a topoisomerase II inhibitor. It effectively inhibits DNA and RNA synthesis, diminishes cancer cell viability, and promotes apoptosis and necrosis. This cytotoxic compound is utilized in researching a range of cancers, such as leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, and Wilms' tumor, as well as infections [1] [2] [4] [5].

Exatecan Intermediate 5 serves as an intermediate in the synthesis of Exatecan (DX-8951), a DNA topoisomerase I (topoisomerase I) inhibitor with an IC50 of 2.2 μM (0.975 μg/mL), utilized in cancer research. This intermediate is also employed in the production of Antibody-Drug Conjugates (ADCs).