dna topoisomerase i

Topoisomerase I Inhibitor 9 (compound 3d), a specific inhibitor of leishmanial topoisomerase IB, exhibits antileishmanial activity, demonstrating an IC50 value of 34.81μM against L. donovani promastigotes [1].

Compound 13, a topoisomerase I inhibitor 10, selectively inhibits leishmanial topoisomerase IB and exhibits antileishmanial activity. Specifically, it demonstrates efficacy against L. donovani promastigotes with an IC50 value of 27.91 μM [1].

Topoisomerase I inhibitor 5 is an efficient inhibitor of topoisomerase I, with an IC50 value. It effectively disrupts DNA and inhibits the activity of topoisomerase I. Moreover, it can induce apoptosis in MCF-7 cells and arrest the cell cycle at the G1 phase. Topoisomerase I inhibitor 5 also exhibits potency in reversing P-gp-mediated resistance to Adriamycin [1].

Topoisomerase I (Compound ZML-14) inhibitor 3 induces HepG2 cell apoptosis and arrests cell cycle at G2/M phase. Topoisomerase I inhibitor 3 is an inhibitor of topoisomerase I that interact with topoisomerase I-DNA complex [1].

Topoisomerase I inhibitor 2 (ZML-8) is a highly selective DNA topoisomerase I (Top1) inhibitor that inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis with anti-tumor effect [1].

Topoisomerase I/II inhibitor 2 (compound 1a) can significantly reduce the xenograft tumor growth in mice model which can be used in treating liver cancer. Topoisomerase I/II inhibitor 2 is a DNA topoisomerase I/II dual inhibitor. Topoisomerase I/II inhibitor 2 is a potent Topoisomerase inhibitor with IC50 values of 6.83 μM and 9.82 μM for LM9 cells and Huh7 cells [1].

Topoisomerase I inhibitor 6 (Compound 3) is a potent inhibitor of Topoisomerase I that traps the DNA-Top1 cleavage complex and has low cytotoxicity in non-cancerous cell lines. Research value.

Topoisomerase I inhibitor 7 (Compound 8) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 7 significantly inhibits tumor growth (up to 79%) and increases the lifespan (153%) of mice bearing P388 lymphoma transplants.

Topoisomerase I inhibitor 8, a hexacyclic analogue of camptothecin, is also a potent inhibitor of topoisomerase I and is toxic to tumour cells.

Topoisomerase I/II inhibitor 3 (compound 7) is a potent dual inhibitor of topoisomerase I (Topo I) and II (Topo II) . By inhibiting PI3K /Akt/mTOR signaling pathway, Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis . Topoisomerase I/II inhibitor 3 has research value in liver cancer.

Topoisomerase I inhibitor 4 (compound 7a) is a potent inhibitor of topoisomerase I activity. It effectively inhibits the proliferation of various cancer cell lines including HepG2, A549, MCF-7, and HeLa, with IC50 values of 1.20 μM, 2.09 μM, 1.56 μM, and 1.92 μM, respectively. Thus, Topoisomerase I inhibitor 4 holds promise for cancer research applications [1].

Topoisomerase I/II inhibitor 4 is a potent dual inhibitor of topoisomerase I (Topo I) and II (Topo II) with inhibitory effects on cell proliferation, invasion and migration, and induction of apoptosis, and can be used to study hepatocellular carcinoma.

DNA topoisomerase II inhibitor 1 is a potent inhibitor of DNA topoisomerase II that arrests the cell cycle in sub-G1 phase and induces apoptosis with anti-value-added effects.

Doxorubicin hydrochloride (Adriamycin) belongs to the anthracycline class of antibiotics and is an inhibitor of human DNA topoisomerase I/II (IC50=0.8/2.67 μM). Doxorubicin hydrochloride exhibits cytotoxicity and antitumor activity. Doxorubicin hydrochloride reduces the phosphorylation of AMPK and its downstream target protein acetyl coenzyme A carboxylase, and induces apoptosis and 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.

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.

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

CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC).. CL2A-SN-38 is composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a noncleavable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. .

Daniquidone (Batracylin) is a potent dual inhibitor of DNA topoisomerase I and DNA topoisomerase II with cytotoxic and antiproliferative activity that induces DNA fragmentation for the study of neoplasms, immune disorders, and lymphatic disorders.

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

β-Lapachone (ARQ-501) is a specific DNA topoisomerase I inhibitor, and no inhibitory activities against DNA topoisomerase II or ligase.

Doxorubicin (Adriamycin) is a Topoisomerase II (Top2) inhibitor with antineoplastic activity.

Topotecan (NSC-609669) is a Topoisomerase I inhibitor,and is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.

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.

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.

CH-0793076, a hexacyclic camptothecin analog, is an active drug and major metabolite of TP300. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein). CH-0793076 inhibits DNA topoisomerase I (IC50: 2.3 μM).

MC-SN38 is a drug-linker conjugate that pairs the potent microtubule-disrupting agent SN38 with a non-cleavable MC linker, designed for use in antibody drug conjugates (ADCs). SN38, the active metabolite of the Topoisomerase I inhibitor Irinotecan, works by inhibiting DNA synthesis and inducing DNA single-strand breaks.

CL2-SN-38, a part of the antibody-drug conjugate (ADC), can conjugate with the anti-Trop-2-humanized antibody hRS7. SN-38 is an inhibitor of DNA topoisomerase I.

Becatecarin is a water-soluble, diethylaminoethyl analog of the antineoplastic antibiotic rebeccamycin. It intercalates into DNA, stabilizing the DNA-topoisomerase complex. This results in the potent catalytic inhibition of both topoisomerases I and II, initiating DNA cleavage and apoptosis. Becatecarin, alone or in combination with other compounds, has anti-cancer as well as myelosuppressive effects in vivo. It is also a transport substrate of the ATP-binding cassette (ABC) transporter ABCG2.

Propargyl-PEG4-GGFG-DXd is a drug-linker conjugate for antibody-drug conjugates (ADCs), comprising an ADC linker and the DNA topoisomerase I inhibitor known as DXd [1].

MC-GGFG-DX8951 is a drug-linker conjugate designed for antibody-drug conjugation (ADC) that demonstrates antitumor activity through the deployment of DX8951, a DNA topoisomerase I inhibitor, connected using the protease-cleavable MC-GGFG linker[1].

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.

MC-Val-Cit-PAB-Exatecan (MC-Val-Cit-PAB-DX8951) is a conjugate of the DNA topoisomerase I inhibitor DX-8951 and a cathepsin-cleavable antibody-drug conjugate (ADC) linker, designed for targeted cancer therapy applications.

PNU-EDA-Gly5 is a DNA topoisomerase I inhibitor-based oligo-glycine linker-payload used for the synthesis of antibody-drug conjugates (ADCs). It consists of the DNA topoisomerase I inhibitor PNU-159682 and the linker EDA-Gly5.

Rebeccamycin is an antitumor antibiotic+ inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I. It also has a negligible effect on protein kinase C and topoisomerase II.

MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan is an agent-linker conjugate for antibody-drug conjugates (ADCs), incorporating Exatecan, a DNA Topoisomerase I inhibitor (IC 50 = 2.2 μM) [1].

9-Chloromethyl-10-hydroxy-11-F-Camptothecin, a novel derivative of camptothecin, functions as a DNA topoisomerase I (Topo I) inhibitor with potential applications in anticancer research [1].

DBCO-PEG4-GGFG-Dxd is a conjugate used in antibody-drug conjugates (ADCs) exhibiting potent antitumor activity. It incorporates Dxd, a DNA topoisomerase I inhibitor, connected through the cleavable linker DBCO-PEG4-GGFG [1]. This compound functions as a click chemistry reagent, featuring a DBCO group capable of strain-promoted alkyne-azide cycloaddition (SPAAC) with azide-containing molecules.

Groenlandicine is a protoberberine alkaloid from Coptidis Rhizoma. Groenlandicine exhibits moderate inhibitory effect with IC50 value of 154.2 μM for human recombinant aldose reductase (HRAR). Groenlandicine selectively induces topoisomerase I-mediated DN

Afeletecan is a water-soluble camptothecin derivative. Afeletecan stabilizes the topoisomerase I-DNA covalent complex and forms an enzyme-drug-DNA ternary complex. Both the initial cleavage reaction and religation steps are inhibited and subsequent collis

Huanglongmycin N acts as a DNA topoisomerase I inhibitor, demonstrating an EC50 value of 14 μM.

CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC 50 of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein) [1] .

(±)-10-Hydroxycamptothecin (Hydroxy Camptothecine) is an alkaloid isolated from the stem wood of the Chinese tree, Camptotheca acuminata. This compound selectively inhibits the nuclear enzyme DNA topoisomerase, type I. Several semisynthetic analogs of camptothecin have demonstrated antitumor activity.

Topoisomerase I inhibitor. Forms stable DNA-topoisomerase complexes during DNA replication and induces cell cycle arrest in the G2/M phase. Inhibits growth of a range of cancer cell lines in vitro, as well as of ovarian and leukemia tumors in vivo.

Rubitecan (9-Nitrocamptothecin) is a DNA topoisomerase I inhibitor. It inhibits DNA topoisomerase I and increases the fraction of supercoiled DNA in a cell-free assay in a concentration-dependent manner.Rubitecan is a semisynthetic agent related to camptothecin with potent antitumor and antiviral properties.

Irinotecan-d10 Hydrochloride is a deuterated compound of Irinotecan Hydrochloride. Irinotecan Hydrochloride has a CAS number of 100286-90-6. Irinotecan 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.

MC-VA-PAB-Exatecan is an agent-linker conjugate designed for Antibody-Drug Conjugate (ADC) applications, comprising the ADC linker (peptide MC-VA-PAB) and the DNA topoisomerase I inhibitor Exatecan. Synthesis of this conjugate has demonstrated promising antitumor activity [1].

Belotecan (CKD-602 free base) is an inhibitor of DNA topoisomerase I. Belotecan blocks the cell cycle and induces apoptosis and is an antitumour derivative of camptothecin that can be used in cancer research.

Delimotecan is a DNA topoisomerase I inhibitor. Delimotecan had a long terminal half-life of 109 h, and relatively high exposures to T-2513 and SN-38 were obtained. The percentage decrease in WBC and absolute neutrophil count significantly correlated with

XR-5000 is a DNA topoisomerase I and II inhibitor.

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