Big Chemical Encyclopedia

Chemical substances, components, reactions, process design ...

Articles Figures Tables About

Topoisomerase 1/II inhibitors

Topoisomerase enzymes (topoisomerases I and II) are enzymes that control the changes in DNA structure by breaking and rejoining the phosphodiester backbone of DNA strand during the normal cell cycles. Topoisomerases have become popular targets for cancer chemotherapy drugs. [Pg.34]

Most of the compounds exhibited improved anticancer activity in human cancer cell lines compared to the marketed drug etoposide 32. [Pg.36]


BOOS G, STOPPER H (2000) Genotoxicity of several clinically used topoisomerase II inhibitors. Toxicol Lett. 116 7-16. [Pg.81]

Teniposide, a topoisomerase II inhibitor, is administered as an infusion over 30 to 60 minutes to prevent hypotension. The pharmacokinetics are described by a three-compartment model, with an a half-life of 0.75 hours, a (5 half-life of 4 hours, and a terminal half-life of 20 hours. Considerable variability in clearance of teniposide in children has been reported.17 Teniposide has shown activity in the treatment of acute lymphocytic leukemia, neuroblastoma, and non-Hodgkin s lymphoma. Side effects include myelosuppression, nausea, vomiting, mucositis, and venous irritation. Hypersensitivity reactions may be life-threatening. [Pg.1288]

Gorbsky GJ 1994 Cell cycle progression and chromosome segregation in mammalian cells cultured in the presence of the topoisomerase II inhibitors ICRF-187 [(+)-l,2-bis(3,5-dioxopiperazinyl-l-yl)propane ADR-529] and ICRF-159 (Razoxane). Cancer Res 54 1042-1048... [Pg.130]

The potential properties of A. suaveolens Bl. has a source of topoisomerase II inhibitor is open for exploration. The plant probably elaborates aporphine alkaloids because aporphines are known to occur in the genus Artabotrys (2,3), Liriodenine and athero-spermidine from Artabotrys undnatus and artabotrine from Artabotrys zeylanicus abrogated the survival of cancer cells cultured in vitro (4). [Pg.172]

Examples of acridin alkaloids used in therapeutics as antineoplastic agents is amsacrine (Amsa P-D ), which is used for the treatment of acute leukemia in adults and malignant lymphomas, refractory to conventional therapy. Amsacrin is an intercalating agent and topoisomerase II inhibitor. [Pg.188]

Meng LH, Zhang JS, Ding J. Salvicine, a novel DNA topoisomerase II inhibitor, exerting its effects by trapping enzyme-DNA cleavage complexes. Biochem Pharmacol 2001 62 733-741. [Pg.226]

Lung Cancer Etoposide (VP-16) -plant alkaloid, topoisomerase II inhibitor -bone marrow suppression -nausea and vomiting -mucocutaneous effects (mucositis, stomatitis)—increased at higher doses -chemical phlebitis common -hypotension with rapid administration -hypersensitivity reactions -secondary leukemia... [Pg.172]

A potentially interesting application of (acyloxy)methyl ester prodrugs can be found in delivery through skin of antibacterial agents. Nalidixic acid (8.53, R = H), a topoisomerase II inhibitor, showed promising activity in the treatment of antiproliferative skin disorders, notably psoriasis. To improve the... [Pg.460]

The major class of topoisomerase I inhibitors comprise of the camptothecins, while topoisomerase II inhibitors fall into several classes - anthracyclines (e.g. doxorubicin), anthracenediones (mitoxantrone), anthrapyrazoles (bianthrazole), actinomycins (actinomycin D), acridines (m-AMSA), ellipticines (9-hydroxy-ellipticine) and epidophyllotoxins (Etoposide (VP-16) and VM-26). The chemical... [Pg.174]

Larsen AK, Escargueil AE, Skladanowski A. Catalytic topoisomerase II inhibitors in cancer therapy. Pharmacol Tter 2003 99 167-81. [Pg.84]

The scaffold contains several proteins, especially HI in the core and topoisomerase II. Both appear important to the compaction of the chromosome. In fact, the relationship between topoisomerase II and chromosome folding is so vital that inhibitors of this enzyme can kill rapidly dividing cells thus, several drugs used in the treatment of cancer are topoisomerase II inhibitors. [Pg.327]

Robert J, Larsen AK (1998) Drug resistance to topoisomerase II inhibitors. Biochimie 80 247-254... [Pg.87]

The topoisomerase II inhibitors etoposide and teni-poside are semisynthetic derivatives of podophyllo-toxin. They form a complex with topoisomerase II and DNA which results in double-stranded DNA... [Pg.456]

Extensive structure modulations were performed to obtain more potent and less toxic anti-cancer agents, such as etoposide used in the therapy of numerous cancers (Fig. 41) [113], In contrast to podophyllotoxin, etoposide derivatives act as DNA topoisomerase II inhibitors. Tafluposide (F 11782) is an etoposide where both hydroxyl functions of the glycoside moiety are acylated with the pen-tafluorophenoxyacetic acid (Fig. 41). It has been demonstrated that tafiuposide does not act as a pro-drug of etoposide, but through a specific mechanism of interaction with both topoisomerases I and lla [114]. [Pg.589]

In 1993, the effects of selected topoisomerase II inhibitors, antimalarial agents, DNA binders, naphthoquinones, and various other agents on integrase activity in vitro were investigated [46]. [Pg.106]

Concise total syntheses of a promising antiinflammatory agent, epoxyquino-mycin B (66), isolated from amycolatopsis sp. MK299-95F4, and a promising topoisomerase-II inhibitor, BE-10988 (67), isolated from the culture broth of a strain of Actinomycetes, have been accomplished by a DMP-induced oxidation reaction of anilides [129] (Scheme 36). [Pg.238]


See other pages where Topoisomerase 1/II inhibitors is mentioned: [Pg.60]    [Pg.282]    [Pg.1289]    [Pg.1408]    [Pg.1411]    [Pg.1411]    [Pg.296]    [Pg.457]    [Pg.135]    [Pg.174]    [Pg.252]    [Pg.417]    [Pg.32]    [Pg.151]    [Pg.160]    [Pg.456]    [Pg.313]    [Pg.1163]    [Pg.104]    [Pg.106]    [Pg.678]    [Pg.88]    [Pg.943]    [Pg.160]    [Pg.364]    [Pg.214]    [Pg.360]    [Pg.60]   
See also in sourсe #XX -- [ Pg.60 ]

See also in sourсe #XX -- [ Pg.447 ]

See also in sourсe #XX -- [ Pg.717 ]

See also in sourсe #XX -- [ Pg.717 ]

See also in sourсe #XX -- [ Pg.103 ]




SEARCH



DNA topoisomerase II inhibitors

II Inhibitors

Topoisomerase

Topoisomerase inhibitors

Topoisomerases

© 2024 chempedia.info