O. P. Shestak, V. Novikov, N. G. Prokof'eva
Dec 1, 1999
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Journal
Pharmaceutical Chemistry Journal
Abstract
2-Acetylcyclopent-4-ene-l,3-diones (I) are known to exhibit high reactivity [1] and possess a broad spectrmn of biological action [2]. In solution, triketones I represent a mixture of four enolic forms [2]. Two of these forms contain both a carbonyl-conjugated l'-hydroxyethylidene group and the 2-ene-l,4-dione fragment, which makes them structurally similar to cyclopentane-based antitumor antibiotics such as pentenomycins [3, 4] (including sarcomycin [5] used in clinical practice), as well as clavulones, chloro(boromo, iodo)valones, and pimaglandins [6, 7]. As is known, 2-alkyl(aryl)idene derivatives of some 4,5-substituted cyclopent-4-ene-l,3-diones exhibit high antitumor activity in v/tro with respect to ascites sarcoma 180 [8] and cell lines of some malignant human tumors [6]. In this context, it was of interest to study the cytotoxicity of uiketones I a Ih and their sodium salts (II) and deacylated derivatives (ILl).