A doxorubicin analog that demonstrates anti-cancer activity without cardiotoxicity, does not inhibit topoisomerase IIβ activity at 100 uM.

Amonafide(AS1413) produces protein-associated DNA-strand breaks through a topoisomerase II-mediated reaction, but does not produce topoisomerase I-mediated DNA cleavage.

Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic and water-soluble camptothecin derivative.

Beta-Lapachone is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.

Betulinic acid, a pentacyclic triterpene, selectively induces apoptosis in tumor cells, also is a inhibitor of HIV-1 with EC50 of 1.4 μ M.

Camptothecin (CPT) is a potent DNA enzyme topoisomerase I (topo I) inhibitor with an IC50 and IC70 of 50 nM and 0.225 μM for breast cancer cell line MDA-MB-231.

Cytosine β-D-arabinofuranoside hydrochloride is an anti-leukemic agent which binds to topoisomerase I resulting in DNA fragmentation and inhibition of replication. In addition this compound does not have any effects on RNA synthesis. Cytosine β-D-arabinof

Doxorubicin (Adriamycin) is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis.

Ellipticine hydrochloride is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.

Ellipticine is a DNA intercalating agent and a DNA topoisomerase II inhibitor.

Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity.

Genz-644282 is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity(IC50=1.2 nM).

Idarubicin Hcl is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor.

Irinotecan prevents DNA from unwinding by inhibition of topoisomerase 1.

Irinotecan(CPT-11) prevents DNA from unwinding by inhibition of topoisomerase 1.

SN-38(NK-012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks.

SW-044248 is a Novel Inhibitor of Topoisomerase I Is Selectively Toxic for a Subset of Non-Small Cell Lung Cancer Cell Lines.

TAS-103 2Hcl(BMS-247615 2Hcl) is a dual inhibitor of topoisomerase-I (topo-I) and topoisomerase-II (topoII).

TAS-103(BMS-247615) is a dual inhibitor of topoisomerase-I (topo-I) and topoisomerase-II (topoII).

Voreloxin(SNS-595; AG 7352) is a small molecule and a naphthyridine analogue with antineoplastic activity; inhibitor of Topo II.

Epirubicin HCl, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase.

RPR121056 (APC) is a metabolite of Irinotecan (CPT-11), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE.