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topoisomerase II inhibitor
Adriamycin is an anthracycline antibiotic, it works by intercalating DNA, while most serious adverse effect being life-threatening heart damage. It is commonly used in the treatment of a wide range of cancers, including hematological malignancies, many types of carcinoma, and soft tissue sarcomas.
- Sanaz Naghibi, .et al. , Biosensors (Basel), 2022, May 29;12(6):373 PMID: 35735521
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Topoisomerase inhibitor
Amonafide is a DNA intercalator and topoisomerase II inhibitor for the treatment of neoplastic diseases, one of Antitumor agent.
- Veronica Rendo, .et al. , Nat Commun, 2020, 11: 1308 PMID: 32161261
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Topoisomerase I inhibitor
Camptothecin is a cytotoxic quinoline alkaloid which inhibits the DNA enzyme topoisomerase I (topo I). -
Topoisomerase inhibitor
Cerubidine (Daunorubicin HCl, Rubidomycin HCl) interacts with DNA by intercalation and inhibition of macromolecular biosynthesis. This inhibits the progression of the enzyme topoisomerase II, which relaxes supercoils in DNA for transcription. It stabilizes the topoisomerase II complex after it has broken the DNA chain for replication, preventing the DNA double helix from being resealed and thereby stopping the process of replication.
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Topoisomerase II inhibitor
Epirubicin is a cell-permeable anthracycline antitumor antibiotic. It is a stereoisomer(4?€?-epi-isomer) of doxorubicin that exhibits reduced cardiotoxicity. It is used to inhibit topoisomerase II and DNA helicase activity. -
Topoisomerase II inhibitor
Etoposide forms a ternary complex with DNA and the topoisomerase II enzyme (which aids in DNA unwinding), prevents re-ligation of the DNA strands, and by doing so causes DNA strands to break. Therefore, this causes errors in DNA synthesis and promotes apoptosis of the cancer cell.- Bageshri Naimish Nanavati, .et al. , bioRxiv, 2023, Feb 23 PMID: 36865131
- Sibei Wang, .et al. , Molecules, 2023, Jan 19;28(3):1016 PMID: 36770683
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Chen JC, .et al. , Biomolecules, 2019, Sep 9;9(9) PMID: 31505885
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Calhelha RC, .et al. , Analyst, 2017, Oct 23;142(21):4124-4141 PMID: 28991301
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DNA gyrase/topoisomerase IV inhibitor
Gatifloxacin is a fluoroquinolone antibiotic which inhibits bacterial DNA gyrase (IC50 = 0.109 ng/ml) and topoisomerase IV (IC50 = 13.8 ng/ml). -
Topoisomerase inhibitor
Idarubicin is an anthracycline antibiotic that is an anti-leukemia agent with higher DNA binding capacity and greater cytotoxicity than daunorubicin.- Wei Y, .et al. , Mol Cell, 2017, Jun 1;66(5):581-596.e6 PMID: 28552615
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Topoisomerase I inhibitor
Irinotecan prevents DNA from unwinding by inhibition of topoisomerase 1.- Gils Jose, .et al. , Cancers (Basel), 2020, Oct 31;12(11):E3211 PMID: 33142721
- T Kannathasan, .et al. , Cancers (Basel), 2020, May; 12(5): 1231 PMID: 32422901
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Topoisomerase inhibitor
Irinotecan (CPT 11), a compound within the camptothecin family, is an inhibitor of topoisomerase 1 involved in cellular DNA replication and transcription. -
Topoisomerase inhibitor
Marbofloxacin is a potent antibiotic of the 3rd generation fluoroquinolone group and acts by inhibiting bacterial DNA replication. -
Topoisomerase inhibitor
Moxifloxacin is a quinolone/fluoroquinolone antibiotic.- Hiroshi Arakawa, .et al. , Biopharm Drug Dispos, 2016, Jan;37(1):39-45 PMID: 26590007
- Arisa Higa, .et al. , Fundam. Toxicol. Sci, 2016, 3(2): 47-53
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Topoisomerase inhibitor
Norfloxacin(Norxacin) is a broad-spectrum antibiotic. -
Topoisomerase inhibitor
Ofloxacin is a synthetic broad-spectrum antimicrobial agent. -
Topoisomerase II inhibitor
Pirarubicin is an analogue of the anthracycline anti-neoplastic doxorubicin. Intercalates into DNA and interacts with Topo II (topoisomerase II) and supressing DNA replication- Krishna K Ramajayam, .et al. , Int J Hyperthermia, 2022, 39(1):998-1009 PMID: 35876089
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DNA topoisomerase I inhibitor
Topotecan HCl (Hycamtin) is a chemotherapeutic agent that is a topoisomerase inhibitor. -
Topoisomerase inhibitor
Balofloxacin is a quinolone antibiotic. The bactericidal action of Balofloxacin results from interference with the enqyme DNA gyrase which is needed for the synthesis of bacterial DNA. Balofloxacin is efficacious against Gram-negative bacteria. It also has enhanced activity against Gram positive bacteria, including MRSA and Streptococcus pneumoniae. -
Topoisomerase inhibitor
Sarafloxacin hydrochloride is a fluoroquinolone antibacterial agent. Inhibits bacterial DNA gyrase (topoisomerase). -
Topoisomerase II inhibitor
Flumequine is a synthetic chemotherapeutic antibiotic which affecting mammalian chromosome and DNA unwinding at the level of gyrase/topoisomerases. -
Topoisomerase
(S)-10-Hydroxycamptothecin is a camptothecin derivative that inhibits DNA topoisomerase by enacting strand breaks in chromosomal DNA and inducing apoptosis. -
DNA topoisomerase Inhibitor
SN 38 is the active metabolite of irinotecan (an analog of camptothecin - a topoisomerase I inhibitor).- Sarigama Rajesh, .et al. , Pharmaceutics, 2022, Oct 12;14(10):2175 PMID: 36297610
- Chen JC, .et al. , Biomolecules, 2019, Sep 9;9(9) PMID: 31505885
- Alibolandi M, .et al. , Artif Cells Nanomed Biotechnol, 2018, May 27:1-12 PMID: 29806500
- Bar-Zeev M, .et al. , Eur J Pharm Biopharm, 2018, Dec;133:240-249 PMID: 30367935
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Topoisomerase inhibitor
Epirubicin is a cell-permeable antitumor antibiotic. A stereoisomer of Doxorubicin that exhibits reduced cardiotoxicity. Epirubicin?€?s antitumor actions are mediated by targeting and inhibiting Topo II (topoisomerase II).- Xiu-wu Pan, .et al. , Oncol Rep, 2016, Jan;35(1):334-42 PMID: 26496799
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Topoisomerase I inhibitor
9-Aminocamptothecin is a topoisomerase I inhibitor with potent anticancer activity. -
topoisomerase II inhibitor
Ametantrone (AM) is a synthetic 9,10-anthracenedione bearing two (hydroxyethylamino)ethylamino residues at positions 1 and 4 along with other anthraquinones and anthracyclines. -
Topoisomerase II inhibitor
Pixantrone is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity. -
DNA topoisomerase II inhibitor
Beta-Lapachone is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase.- Xiaoling Li, .et al. , ACS Appl. Bio Mater, 2020, 3, 3, 1769-1778
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topoisomerase 1 inhibitor
Genz-644282 is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity. -
human topoisomerase I (Top1) inhibitor
Top1 inhibitor 1 (compound 28) is a potent human topoisomerase I (Top1) inhibitor with an IC50 value of 29 nM. -
Topoisomerase I inhibitor
CKD-602 is a topoisomerase I inhibitor. -
DNA topoisomerase II inhibitor
Ellipticine is a DNA intercalating agent and a DNA topoisomerase II inhibitor.- Calhelha RC, .et al. , Analyst, 2017, Oct 23;142(21):4124-4141 PMID: 28991301
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Topoisomerase II inhibitor
NK314 is a novel synthetic benzo[c]phenanthridine alkaloid that shows strong antitumor activity. It inhibited topoisomerase II activity and stabilized topoisomerase II-DNA cleavable complexes.- Kopa P, .et al. , Mol Biol Rep, 2019, Oct 3 PMID: 31583565
- Macieja A, .et al. , Mol Biol Rep, 2019, Apr 24 PMID: 31020489
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topoisomerase I/II inhibitor
TAS 103, also known as BMS-247615, is a quinoline derivative that displays antitumor activity in murine and human tumor models -
Topoisomerase II inhibitor
Nemorubicin is an anticancer drug with IC50 value of 0.08 uM. It is active on tumors resistant to alkylating agents, topoisomerase II inhibitors and platinum derivatives. It works primarily through topoisomerase I inhibition. -
Topoisomerase II inhibitor
Doxorubicin is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis.- Laura Wiggins, .et al. , Nat Commun, 2023, 14: 1854
- Stefania Scialla, .et al. , Int J Pharm, 2023, Feb 5;632:122575 PMID: 36603672
- Fernando Espinola-Portilla, .et al. , Mol. Pharmaceutics, 2023, 20(3): 1490-1499
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- R Mahalakshmi, .et al. , Mol Biol Rep, 2022, Jan;49(1):463-476 PMID: 34739690
- J Priyanga, .et al. , Chem Biol Interact, 2020, Nov 1;331:109250 PMID: 32956706
- Abdelrehim A, .et al. , PLoS One, 2019, Feb 22;14(2):e0212701 PMID: 30794671
- J Wei, .et al. , bioRxiv, 2018, 2018
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Topoisomerase inhibitor
Voreloxin Hcl is a small molecule and a naphthyridine analogue with antineoplastic activity; inhibitor of Topo II. -
topoisomerase II IV inhibitor
Levofloxacin is a broad-spectrum, third-generation fluoroquinolone antibiotic and optically active L-isomer of ofloxacin with antibacterial activity. -
DNA gyrase and topoisomerase IV inhibitor
Clinafloxacin is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae. -
topoisomerase IV inhibitor
Ciprofloxacin hydrochloride is a broad-spectrum antimicrobial carboxyfluoroquinoline, an fluoroquinolone antibiotic that is widely used as an antimicrobial and immunomodulatory agent -
topoisomerase II inhibitor
Amsacrine hydrochloride (m-AMSA hydrochloride; acridinyl anisidide hydrochloride) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells. -
topoisomerase IIα inhibitor
Dexrazoxane is an intracellular iron chelator and an inhibitor of topoisomerase IIα. -
Topoisomerase I inhibitor
Belotecan, also known as CKD-602, is the semi-synthetic camptothecin analogue belotecan with potential antitumor activity. -
topoisomerase II inhibitor
Pirarubicin Hydrochloride is an anthracycline antibiotics, acts as a topoisomerase II inhibitor, and is a widely used for treatment of various cancers, in particular, solid tumors.
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