Synthesis and biological evaluation of rebeccamycin analogues modified at the imide moiety.

Autor: Animati F; Menarini Ricerche Pomezia, via Tito Speri 10, 00040 Pomezia (Rome), Italy., Berettoni M, Bigioni M, Binaschi M, Cipollone A, Irrissuto C, Nardelli F, Olivieri L
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Aug 01; Vol. 22 (15), pp. 5013-7. Date of Electronic Publication: 2012 Jun 15.
DOI: 10.1016/j.bmcl.2012.06.016
Abstrakt: Glycosylated indolocarbazoles related to the antibiotic rebeccamycin represent an important class of antitumour drugs. In the course of our structure-activity relationship studies, new rebeccamycin analogues modified at the imide moiety were synthesised. The antiproliferative activity of the compounds was evaluated on three human cancer cell lines, A2780 (ovarian cancer), H460 (lung cancer), and GLC4 (small-cell lung cancer). The in vitro cytotoxicity of compounds 2 and 4, characterised respectively by a 1,3-dioxolan and (1,3-dioxolan-4-yl)methylene groups linked to the imide moiety, was higher than the reference compound, edotecarin. The effect of compound 2 in inducing tumour regression in the A2780 xenograft model was also investigated.
(Copyright © 2012 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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