Preparation, characterization and the anticancer activity of a novel series of triaminemonochloroplatinum(II) cations linked to anthraquinone intercalators

Autor:	R. Ben-Shoshan, Dan Gibson, Israel Ringel, J. Katzhendler, K.-F. Gean, Avner Ramu
Rok vydání:	1991
Předmět:	Pharmacology Denticity Stereochemistry Organic Chemistry Intercalation (chemistry) Ethylenediamine General Medicine Chemical synthesis Anthraquinone chemistry.chemical_compound chemistry Covalent bond Drug Discovery Linker Cis–trans isomerism
Zdroj:	European Journal of Medicinal Chemistry. 26:593-598
ISSN:	0223-5234
DOI:	10.1016/0223-5234(91)90193-q
Popis:	A new series of complexes of the type [PtAm2LCl]+ (where Am = NH3 or Am2 = ethylenediamine and L is a monodentate AQ-Y-(CH2)n-NH2, AQ = anthraquinone, Y = NH, O) was prepared and screened in vitro against P388 leukemia. These complexes displayed higher activities than the corresponding neutral PtAm2L2 1:2 Pt:anthraquinone complexes but lower than the neutral diaminedichloro 1:1 complexes. The [Pt(en)LCl]+ complexes were significantly less active than the cis- and trans-[Pt(NH3)2LCl]+ complexes. The cis and trans isomers displayed similar activities. The complexes bearing the shorter linker chains were more active than those with longer chains. In vivo toxicity studies indicate that they are significantly less toxic than cis-DDP.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::e3483be39628a94e864f9f7d93126764 https://doi.org/10.1016/0223-5234(91)90193-q Zobrazit plný text záznamu