Naphthazarin derivatives (II): formation of glutathione conjugate, inhibition of DNA topoisomerase-I and cytotoxicity

Autor:	G Y, Song, X G, Zheng, Y, Kim, Y J, You, D E, Sok, B Z, Ahn
Rok vydání:	1999
Předmět:	Structure-Activity Relationship Tumor Cells Cultured Animals Antineoplastic Agents Enzyme Inhibitors Topoisomerase I Inhibitors Leukemia L1210 Glutathione Naphthoquinones
Zdroj:	Bioorganicmedicinal chemistry letters. 9(16)
ISSN:	0960-894X
Popis:	6-(1-Hydroxyalkyl)-5,8-dimethoxy-1,4-naphthoquinones, expressing a higher reactivity in conjugation with glutathione, showed a greater potency in the inhibition of DNA topoisomerase-I and the cytotoxicity against L1210 cells than 2-(1-hydroxyalkyl)-DMNQ derivatives, implying the participation of electrophilic arylation in the bioactivities. In further study 6-(1-Hydroxyalkyl)-5,8-dimethoxy-1,4-naphthoquinones with an alkyl group of shorter chain length (C2-C6) exerted a greater bioactivities than those with longer chain length(C6).
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid________::7283936b21e3615610f8f11eac0e1951 https://pubmed.ncbi.nlm.nih.gov/10476878 Zobrazit plný text záznamu Full Text from ScienceDirect