topoisomerase i

TopoisomeraseI/II inhibitor 6 (compound 3i) acts as an effective inhibitor of topoisomerase I and II, with IC50 values of 4.77 µM and 15 µM, respectively. Additionally, it exhibits antiproliferative activity against the human melanoma cell line LOX IMVI, demonstrating IC50 values of 26.7 µM and 25.4 µM.

Compound 5h (Topoisomerase I/II inhibitor 7) is a Topoisomerase I/II inhibitor.

Topoisomerase I inhibitor 14 (Compound 4h) acts as an inhibitor of topoisomerase I. It suppresses the proliferation of A549 and C6 cells, with IC50 values of 4.56 μM and 13.17 μM, respectively. The compound shows no significant toxicity towards healthy NIH3T3 cells (IC50 of 74.44 μM) and demonstrates anticancer activity.

TopoisomeraseI inhibitor 12 (compound 12) is a Camptothecin-derived compound and serves as a potent inhibitor of Topoisomerase I (TopoisomeraseI). This compound exhibits anticancer properties.

TopoisomeraseI inhibitor 15 (compound 4b) is an inhibitor of topoisomerase I, exhibiting anticancer properties. Its IC50 value against A549 cells is 7.34 μM.

Topoisomerase I inhibitor 21 (Compound 3e) inhibits Topoisomerase I by stabilizing the enzyme-DNA complex. It exhibits antiproliferative activity in 39 types of human cancer cells (JFCR39), with an average GI50 of 39 nM.

TopoisomeraseI/II-IN-1 is a dual inhibitor of Topoisomerase I and II. It induces G2/M cell cycle arrest and apoptosis (apoptosis) in cancer cells by increasing the levels of p53, p21, Bax mRNA, and caspase-3 proteins, as well as the Bax/Bcl-2 ratio, while decreasing Bcl-2 levels. This compound is useful for research on various cancers such as melanoma, renal cancer, colorectal cancer, and breast cancer.

Topoisomerase I inhibitor 2 (ZML-8) is a highly selective DNA topoisomerase I (Top1) inhibitor that impedes Top1 activity, causing DNA damage. It arrests the cell cycle at the G2/M phase and induces apoptosis, exhibiting anti-tumor effects [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/II inhibitor 2 (compound 1a) is a DNA topoisomerase I/II dual inhibitor that significantly reduces xenograft tumor growth in a mouse model, indicating its potential use in treating liver cancer. It 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 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 I inhibitor 4 (compound 7a) is a potent inhibitor of topoisomerase I activity, effectively inhibiting 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 3 (compound 7) is a potent dual inhibitor of topoisomerase I (Topo I) and II (Topo II) that inhibits the PI3K/Akt/mTOR signaling pathway, subsequently inhibiting cell proliferation, invasion, and migration, and inducing apoptosis. This compound has research value in liver cancer.

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

Topoisomerase I inhibitor 6 (Compound 3) is a potent Topoisomerase I inhibitor that traps the DNA-Top1 cleavage complex and exhibits low cytotoxicity in non-cancerous cell lines, making it valuable for research.

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 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.

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 11 effectively inhibits Topoisomerase I and has the capability to bind to BTK [1].

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

TopoisomeraseI inhibitor 17 (Compound 7h) is an inhibitor of TopoisomeraseI (Top1). It reduces DDX5 and reverses the locking effect of DDX5 on Top1 activity. This compound induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. It triggers apoptosis by decreasing anti-apoptotic proteins XIAP, Bcl-2, and Survivin, while increasing pro-apoptotic proteins Bax and γH2AX. Moreover, TopoisomeraseI inhibitor 17 halts progression at the G2/M checkpoint, leading to cell cycle arrest. It significantly impairs colorectal cancer cell colony formation and migration, and effectively reduces tumor size in human PDX tumor mouse models.

TopoisomeraseI/II inhibitor 8 (Compound Ru7) is a dual catalytic inhibitor of TopoisomeraseI/II that induces DNA damage and activates PARP-1, leading to the activation of RIPK1, RIPK3, and MLKL, ultimately causing necroptosis. It shows significant anticancer activity by effectively targeting cancer cell nuclei and inducing cell death through necroptosis, offering substantial clinical potential in overcoming resistance in cancer treatment.

TopoisomeraseI inhibitor 13 (Compound G11) is a Topo I inhibitor that effectively blocks the proliferation of cancer cells and significantly inhibits tumor growth in vivo.