topo i

DRF-1042 HCl is an orally active camptothecin analog with antitumor activity, inhibits DNA topoisomerase I, and is used in the study of refractory solid tumors.

Simmitecan hydrochloride is a camptothecin derivative, a topoisomerase I inhibitor with anticancer activity, which can be used to study is solid tumors.

Ellagic acid (Gallogen), a thickened tetracyclic natural product, is a potent CK2 inhibitor (IC50=40 nM; Ki=20 nM) with ATP-competitive properties. Ellagic acid is an antioxidant and also possesses antiproliferative activity.

Irinotecan hydrochloride trihydrate (CPT-11 HCl Trihydrate) keeps DNA from unwinding by inhibiting topoisomerase 1.

Irinotecan Hydrochloride (CPT-11 hydrochloride) is the hydrochloride salt of a semisynthetic derivative of camptothecin. Irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Because ongoing DNA synthesis is necessary for irinotecan to exert its cytotoxic effects, it is classified as an S-phase-specific agent.

Novobiocin Sodium (Albamycinsodium) binds to DNA gyrase and blocks adenosine triphosphatase (ATPase) activity. Novobiocin sodium is an antibiotic compound derived from Streptomyces niveus. It has a chemical structure similar to coumarin.

Camptothecin (CPT) belongs to the alkaloid group of natural products and is a specific DNA topoisomerase I (Topo I) inhibitor (IC50=679 nM) with specificity. Camptothecin has antitumor activity and induces apoptosis.

SN-38 (NK012) is the active metabolite of Irinotecan, a DNA topoisomerase I (Topo I) inhibitor, which inhibits DNA and RNA synthesis (IC50=0.077/1.3 μM). SN-38 has antitumor activity and induces autophagy.

Sophoridine (Dihydro-5-episophocarpine), a natural anticancer drug, has been used in China for decades. A series of novel N-substituted Sophoridinic acid derivatives were synthesized and evaluated for their cytotoxicity with 1 as the lead. The structure-activity relationship indicated that introduction of an aliphatic acyl on the nitrogen atom might significantly enhance the anticancer activity. Among the compounds, 6b bearing bromoacetyl side-chain afforded a potential effect against four human tumor cell lines (liver, colon, breast, and lung). The mechanism of action of 6b is to inhibit the activity of DNA topoisomerase I, followed by the S-phase arrest and then cause apoptotic cell death, similar to that of its parent 1.

Irinotecan (CPT-11), a derivative of camptothecin, is an inhibitor of DNA topoisomerase I (Topo I). Irinotecan has antitumor activity by preventing DNA strand reattachment through binding to the Topo I complex, resulting in double-stranded DNA breaks and cell death.

Aclacinomycin A (Aclarubicin) is a novel anthracycline antibiotic isolated from Streptomyces galilei with antitumor activity.Aclacinomycin A is an inhibitor of topoisomerases I and II and inhibits RNA activity.Aclacinomycin A has been used in the study of relapsed leukemia and advanced malignant lymphomas.

9-amino-CPT (Aminocamptothecin) is an inhibitor of topoisomerase I with potent anticancer activity.

9-Hydroxycampothecin is a camptothecin derivative with anticancer activity.

Belotecan hydrochloride (CKD-602) is a synthetic water-soluble camptothecin derivative and topoisomerase I inhibitor with potential antitumor activity

(rac)-Exatecan Intermediate 1 is a camptothecin derivative, a potential topoisomerase I inhibitor, used in tumor research.

12-Ethyl-9-hydroxycamptothecin (SN38) is the active metabolite of irinotecan, a topoisomerase I inhibitor, with potential anticancer activity for use in the study of colon and rectal cancer.

Exatecan Mesylate (DX8951f) is a DNA topoisomerase I inhibitor (IC50: 2.2 μM, 0.975 μg/mL).

Podocarpusflavone A is a DNA topoisomerase I inhibitor with moderate anti-proliferative activity that induces cell apoptosis in MCF-7.

LMP744 hydrochloride (NSC-706744 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity. 

Topo I II-IN-1 (compound 7t) is an effective dual inhibitor of Topo I and Topo II. It exhibits significant cytotoxicity against the MCF-7 breast cancer cell line, with an IC50 value of 7.45 μM.

Topo I II-IN-2 (Compound 3g) is an inhibitor of both Topo I and Topo II. It exhibits inhibitory activity against NCI-H446 and NCI-H1048 cells with IC50 values of 1.30 μM and 1.42 μM, respectively. Topo I II-IN-2 induces mitochondrial apoptosis, disrupts mitochondrial function, and stimulates activity generation. Additionally, it inhibits the PI3K Akt mTOR pathway, effectively preventing the proliferation, invasion, and migration of small cell lung cancer (SCLC) cells in vitro.

Topo I COX-2-IN-1 (1H-30) is a potent Topo I COX-2 inhibitor with IC50 values of 0.24 μM for COX-2 and 4.42 μM for Topo I. It induces apoptosis and inhibits cancer cell migration, demonstrating anti-cancer activity.

Topo I-IN-1 (Compound 14d) is a potent Topo I inhibitor that exhibits antitumor activity, DNA intercalative capability, and can induce cell apoptosis.

Topo I COX-2-IN-2 (Compound W10) is a potent dual inhibitor of Topo I (IC50: 0.90 μM) and COX-2 (IC50: 2.31 μM), inducing apoptosis in cancer cells via the mitochondrial pathway.