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Design, synthesis and topoisomerase II inhibition activity of 4'-demethylepipodophyllotoxin-lexitropsin conjugates.
Anticancer Drug Des. 1996 Jun; 11(4):325-38.AD

Abstract

The design and synthesis of 4'-demethylepipodophyllotoxin-lexitropsin conjugates capable of inhibiting the actions of topoisomerase II are described. Siteselective topoisomerase II cleavage was observed in the presence of the new inhibitors, as determined by DNA sequencing. Additional topoisomerase II cleavage sites were observed with the new compounds that seem to be characteristic of the minor groove-binding lexitropsin moieties. Compound 17, having three pyrrole units in its binding moiety, exhibited distinct topoisomerase-mediated sites of cleavage at positions 4258, 4257, 4255 and 4247 of the pBR322 DNA fragment. These results demonstrate that conjugation with minor groove-binding moieties can alter or increase the number of topoisomerase II-induced cleavable sites and contribute to our understanding of the cytostatic activity of these compounds against KB cancer cell lines.

Authors+Show Affiliations

Department of Chemistry, University of Alberta, Edmonton, Canada.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

8679055

Citation

Gupta, R, et al. "Design, Synthesis and Topoisomerase II Inhibition Activity of 4'-demethylepipodophyllotoxin-lexitropsin Conjugates." Anti-cancer Drug Design, vol. 11, no. 4, 1996, pp. 325-38.
Gupta R, al-Said NH, Oreski B, et al. Design, synthesis and topoisomerase II inhibition activity of 4'-demethylepipodophyllotoxin-lexitropsin conjugates. Anticancer Drug Des. 1996;11(4):325-38.
Gupta, R., al-Said, N. H., Oreski, B., & Lown, J. W. (1996). Design, synthesis and topoisomerase II inhibition activity of 4'-demethylepipodophyllotoxin-lexitropsin conjugates. Anti-cancer Drug Design, 11(4), 325-38.
Gupta R, et al. Design, Synthesis and Topoisomerase II Inhibition Activity of 4'-demethylepipodophyllotoxin-lexitropsin Conjugates. Anticancer Drug Des. 1996;11(4):325-38. PubMed PMID: 8679055.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Design, synthesis and topoisomerase II inhibition activity of 4'-demethylepipodophyllotoxin-lexitropsin conjugates. AU - Gupta,R, AU - al-Said,N H, AU - Oreski,B, AU - Lown,J W, PY - 1996/6/1/pubmed PY - 1996/6/1/medline PY - 1996/6/1/entrez SP - 325 EP - 38 JF - Anti-cancer drug design JO - Anticancer Drug Des. VL - 11 IS - 4 N2 - The design and synthesis of 4'-demethylepipodophyllotoxin-lexitropsin conjugates capable of inhibiting the actions of topoisomerase II are described. Siteselective topoisomerase II cleavage was observed in the presence of the new inhibitors, as determined by DNA sequencing. Additional topoisomerase II cleavage sites were observed with the new compounds that seem to be characteristic of the minor groove-binding lexitropsin moieties. Compound 17, having three pyrrole units in its binding moiety, exhibited distinct topoisomerase-mediated sites of cleavage at positions 4258, 4257, 4255 and 4247 of the pBR322 DNA fragment. These results demonstrate that conjugation with minor groove-binding moieties can alter or increase the number of topoisomerase II-induced cleavable sites and contribute to our understanding of the cytostatic activity of these compounds against KB cancer cell lines. SN - 0266-9536 UR - https://www.unboundmedicine.com/medline/citation/8679055/Design_synthesis_and_topoisomerase_II_inhibition_activity_of_4'_demethylepipodophyllotoxin_lexitropsin_conjugates_ L2 - https://www.lens.org/lens/search?q=citation_id:8679055 DB - PRIME DP - Unbound Medicine ER -