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DNA topoisomerase II inhibitors

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]

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]

C. M., Makaluvamines, marine natural products, are active anti-cancer agents and DNA topoisomerase II inhibitors, Anti-Cancer Drug Design, 8, 333, 1993. [Pg.538]

Pommier, Y. (1997) DNA topoisomerase II inhibitors, in Cancer Therapeutics Experimental and Clinical Agents (Teicher, B. A., ed.), Humana Press, Totowa, NJ, pp. 153-174. [Pg.109]

Duca el al. [45] synthesized a series of 4-/0-amino-4 -O-demethyl-4-desoxy-podophyllotoxins (XIX) as DNA topoisomerase II inhibitors and also evaluated their cytotoxicities against L1210 cell line. From the cytotoxic data of these compounds, we developed Eq. 21 (Table 8) ... [Pg.76]

C32H32O13S 656.663 Closely related to Etoposide, E-31. DNA topoisomerase II inhibitor. Antineo-plastic agent. Used in combination therapies. Cryst. (EtOH). Mp 242-246°. [a]g -107 (CHCU/MeOH). Log P -0.75 (uncertain value) (calc). [Pg.901]

Kasahara, K., Fujiwara, Y., Sugimoto, Y, Nishio, K., Tamura, T., Matsuda, T., Saijo, N. 1992. Determinants of response to the DNA topoisomerase II inhibitors doxorubicin and etoposide in human lung cancer cell lines, / Natl. Cancer Inst. 84 113-118. [Pg.8]

MARKOVITS J, LINASSIER C, FOSSE P, COUPRIE J, PIERRE J, JACQUEMIN-SABLON A, SAUCIER J M, LE PECQ J B, LARSEN A K (1989) Inhibitory effects of the tyrosine kinase inhibitor genistein on mammalian DNA topoisomerase II. Cancer Res. 49 5111-17. [Pg.83]

Downes CS, Mullinger AM, Johnson RT 1991 Inhibitors of DNA topoisomerase II prevent chromatid separation in mammalian cells but do not prevent exit from mitosis. Proc Nad Acad Sci USA 88 8895-8899... [Pg.129]

Substances known as intercalators, such as rifamycin and actinomycin D (bottom) are deposited in the DNA double helix and thereby interfere with replication and transcription (B). As DNA is the same in all cells, intercalating antibiotics are also toxic for eukaryotes, however. They are therefore only used as cytostatic agents (see p. 402). Synthetic inhibitors of DNA topoisomerase II (see p. 240), known as gyrase inhibitors (center), restrict replication and thus bacterial reproduction. [Pg.254]

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]

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]

Combining this pyrroloiminoquinone formation [58,122], the cyclic sulfide formation of phenol ether 159 using PIFA-BF3 Et20 [59], and a-azidonation of cyclic sulfide (160) using Phl=0-TMSN3 [123], the first total synthesis of ( )-makaluvamine F (57), which is a potent inhibitor for DNA topoisomerase II, was achieved by Kita and co-workers [124,125] (Scheme 31). [Pg.236]

As reported by Apers et al. [89], podophyllotoxin derivatives can be divided into two groups in terms of their mechanism of action 1 Inhibitors of tubulin polymerization (such as podophyllotoxin), 2 Inhibitors of DNA topoisomerase II (such as etoposide and teniposide). Combining both pharmacophores leads to compounds with a dual mechanism of action, such as azatoxin. [Pg.136]

THY-R, thyroid hormone receptor TIMP, tissue inhibitor of metalloprotease TK, tyrosine kinase TLC, thin layer chromatography TLRs, Toll-like receptors TMAOX, trimethylamine oxidase TMY tobacco mosaic virus TNF, tumour necrosis factor TNF-a, tumour necrosis factor-a TNF-a-RTK, tumour necrosis factor-a receptor tyrosine kinase TOPI, DNA topoisomerase I TOPII, DNA topoisomerase II t-PA, tissue plasminogen activator TPA, 12-Tetradecanoylphorbol 13-acetate... [Pg.846]


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See also in sourсe #XX -- [ Pg.76 ]




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Topoisomerase II inhibitors

Topoisomerase inhibitors

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