|Zabofloxacin, also known as DW-224; DW-224a; PB-101, is DNA topoisomerase IV inhibitor potentially for the treatment of chronic obstructive pulmonary disease. Zabofloxacin shows activity for multidrug-resistant infections due to Gram-positive bacteria. Zabofloxacin has a broad spectrum of antimicrobial activity, which is especially potent against Gram-positive bacteria.
|Voacamine, isolated from the plant Tabernaemontana coronaria, is an antiprotozoal agent effective against a large array of trypanosomatid parasites including Indian strain of Leishmania donovani and Brazilian strains of Leishmania amazonensis and Trypanosoma cruzi by inhibiting the relaxation activity of topoisomerase IB.
|Trovafloxacin is a broad spectrum antibiotic that inhibits the uncoiling of supercoiled DNA in bacteria by blocking the activity of topoisomerase IV (IC50 = 3.02 µg/ml) and DNA gyrase (IC50 = 7.13 µg/ml).
|Top-Tdp Tri Inhibitor C12
|Top-Tdp tri inhibitor C12 is one of the first triple inhibitors of human topoisomerase 1, tyrosyl–DNA phohosphodiesterase 1 (Tdp1), and tyrosyl–DNA phosphodiesterase 2 (Tdp2).
|SN-38 is an active metabolite of CPT-11 that inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks.
|Sabarubicin is a Top II inhibitor with anticancer activity.
|Pixantrone is an experimental antineoplastic drug.
|PEN-866 is a novel esterase-cleavable conjugate of an HSP90i and a topoisomerase I inhibitor.
|NSC745887 can effectively inhibit the proliferation of various cancers by trapping DNA-topoisomerase cleavage. NSC745887 reduced the cell survival rate and increased the sub-G1 population in dose- and time-dependent manners in GBM cells. Moreover, NSC745887 increased expression of γH2AX and caused DNA fragmentation leading to DNA damage.NSC745887 caused apoptosis by the caspase-8/9-caspase-3-poly(ADP-ribose) polymerase cascade.
|NISC-6 is a napthalamide-isoselenocyanate compound which acts as a dual Topoisomerase-IIα and Akt pathway inhibitor.
|Nalidixic acid sodium salt, a quinolone antibiotic, is effective against both gram-positive and gram-negative bacteria. Nalidixic acid acts in a bacteriostatic manner in lower concentrations and is bactericidal in higher concentrations. Nalidixic acid inhibits a subunit of DNA gyrase and topoisomerase IV and reversibly blocks DNA replication in susceptible bacteria.
|Levofloxacin HCl, a fluoroquinolone antibiotic, is an inhibitor of DNA gyrase and topoisomerase IV.
|Irinotecan is a camptothecin analog prevents DNA from unwinding by inhibition of topoisomerase 1.
|(S)-4,11-Diethyl-4-hydroxy-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl [1,4'-bipiperidine]-1'-carboxylate hydrochloride
|Irinotecan HCl is an inhibitor of topoisomerase 1 that prevents DNA from unwinding.
|Intoplicine is a DNA topoisomerase I and II inhibitor potentially for the treatment of cancer.
|Indotecan is a potent topoisomerase 1(Top1) inhibitor with IC50 values of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively.
|Idarubicin is a semisynthetic 4-demethoxy analogue of the antineoplastic anthracycline antibiotic daunorubicin.
|Gepotidacin is a first in class triazaacenaphthylene antibiotic that inhibits bacterial type II DNA replication by inhibiting the activity of bacterial topoisomerase and has in vitro activity against susceptible and drug-resistant pathogens.
|Gemifloxacin mesylate inhibits activities of DNA gyrase and topoisomerase IV, thereby inhibiting DNA replication and eventually bacterial growth.
|Etoposide phosphate disodium
|Etoposide phosphate disodium (BMY-40481 disodium) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate disodium is the phosphate ester prodrug of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate disodium induces cell cycle arrest, apoptosis, and autophagy.
|Ellipticine HCl is a potent antineoplastic agent and inhibits DNA topoisomerase II activities.
|Coralyne is a cytotoxic agent trageting topoisoerase I, used in combinational chemotherapy to improve the effectiveness in combating proliferation of cancer cells.
|Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation and H+ K+-ATPase activity.
|BNP 1350 is a topoisomerase I inhibitor, with potent anti-cancer activity.
|Berubicin hydrochloride is the hydrochloride salt of the anthracycline derivative berubicin with potential antineoplastic activity.
|Belotecan hydrochloride, a synthetic and water-soluble camptothecin derivative, is inhibitor of topoisomerase I.
|Banoxantrone dihydrochloride is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
|Alternariol is a mycotoxin, topoisomerase I and II inhibitor and potential ER agonist found in Alternaria.
|Aldoxorubicin, also known as INNO-206 and Doxo-EMCH, is the 6-maleimidocaproyl hydrazone derivative prodrug of the anthracycline antibiotic doxorubicin with antineoplastic activity. INNO-206 binds selectively to the cysteine-34 position of albumin via its maleimide moiety. Doxorubicin is released from the albumin carrier after cleavage of the acid-sensitive hydrazone linker within the acidic environment of tumors and, once located intracellularly, intercalates DNA, inhibits DNA synthesis, and induces apoptosis. Albumin tends to accumulate in solid tumors as a result of high metabolic turnover, rapid angiogenesis, hyervasculature, and impaired lymphatic drainage. Because of passive accumulation within tumors, this agent may improve the therapeutic effects of doxorubicin while minimizing systemic toxicity.
|AEZS-108 is a peptide agonist of the gonadotropin releasing hormone-1 receptor (GnRH-1R).
|Aclarubicin is an oligosaccharide anthracycline antineoplastic antibiotic isolated from the bacterium Streptomyces galilaeus.
|Aclacinomycin A HCl
|Aclarubicin HCl is the HCl salt of aclarubicin, an oligosaccharide anthracycline antineoplastic antibiotic isolated from the bacterium Streptomyces galilaeus.
|3-O-trans-p-Coumaroyltormentic acid, a natural product isolated and purified from the leaves of Eriobotrya japonica calli, induces apoptotic cell death in human leukemia (HL60) via mainly mitochondrial pathway by, at least in part, Topo I inhibition, and may be promising lead compound for developing an effective drug for treatment of leukemia.
|(±)-10-Hydroxycamptothecin is an inhibitor of topoisomerase I and can affect phosphorylation of histone H1 and H3 with anticancer activity. It can be isolated from camptotheca acuminate.