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7-(3'-Hydroxymethyl-3'-methylallyloxy)coumarin, bearing a 3'-hydroxy-3'-methylallyl group as the O-side chain, and lomatiol, a lapachol derivative sharing the same structural feature, were tested for their in vitro growth inhibitory activities on six cancer cell lines using the MTT colorimetric assay, along with the respective 3',3'-dimethylallyl derivatives and unprenylated products used for comparison. Data revealed that lomatiol displayed the strongest growth inhibitory activities in vitro although not as efficient as the parent compound lapachol. The oxidized O-prenylcoumarin recorded better growth inhibitory capacities than the prenylated and unprenylated parent products., SCOPUS: ar.j, info:eu-repo/semantics/published

Juglone 1 an plumbagin 2 are plant secondary metabolites nowadays well known for their anticancer properties. In this study we synthesized analogues of 1 and 2 deriving from the functionalization of the OH group in position 5 with different side chains in form of esters and ethers. Therefore the growth inhibitory activities of these adducts were evaluated in vitro on six cancer cell lines using the MTT colorimetric assays along with the two natural parent compounds. The data revealed that these latter displayed the strongest growth inhibitory activities in vitro. Quantitative videomicroscopy analyses were then carried out on human U373 glioblastoma cells, which are characterized by various level of resistance to pro-apoptotic stimuli. We compared the naturally occurring reference compounds 1 and 2 with the derivatives exerting the best activities in terms of IC50 growth inhibitory values. These analyses showed that both juglone and plumbagin had a cytostatic effect on U373 cells and were able to overcome the intrinsic resistance of U373 cancer cells to pro-apoptotic stimuli., SCOPUS: ar.j, info:eu-repo/semantics/published

Journal Article, Research Support, Non-U.S. Gov't, SCOPUS: ar.j, info:eu-repo/semantics/published

Three naturally occurring oxyprenylated diketopiperazines were synthesized and preliminarily tested as growth inhibitory agents in vitro against various cancer cell lines. The compounds were tested on six human cancer cell lines with different sensitivity to proapoptotic stimuli using the MTT colorimetric assay. The data revealed that of the chemicals under study only deoxymicelianamide (11) displayed the highest activity, recording mean IC50 growth inhibitory values ranging from 2 to 23 μM. A comparative study with the non-geranylated saturated derivative of (11) revealed the importance of the presence of the geranyloxy side chain and the exocyclic 2,5-DPK double bond moiety for the observed activity. © 2014 Elsevier B.V., SCOPUS: ar.j, info:eu-repo/semantics/published

Lapachol is a naturally occurring 1,4-naphthoquinone originally isolated by the Italian phytochemist E. Paterno from Tabebuia avellanedae (Bignoniaceae) in 1882 and subsequently found in several other genera belonging to the families of Leguminosae, Malvaceae, Plumbaginaceae, Lamiaceae, Arecaceae, Scrophulariaceae, Verbenaceae, Celastraceae, Avicenniaceae, Caesalpiniaceae, Rubiaceae, and Proteaceae. A wide range of pharmacological activities have been observed for lapachol and its semi-synthetic derivatives in the literature, such as antileishmanial, anticarcinomic, anti-inflammatory, antimalarial, antiseptic, antitumor, antiviral, bactericidal, fungicidal, insectifugal, pesticidal, schistosomicidal, termiticidal, and viricidal effects. The aim of this review is to discuss in detail the phytochemical properties and pharmacological effects of the title compound that have been reported thus far, highlighting its potential therapeutic benefits for the future. © 2013 Springer Science+Business Media., SCOPUS: re.j, SCOPUS: re.j, info:eu-repo/semantics/published

Lapachol is a naturally occurring 1,4-naphthoquinone originally isolated by the Italian phytochemist E. Paterno from Tabebuia avellanedae (Bignoniaceae) in 1882 and subsequently found in several other genera belonging to the families of Leguminosae, Malvaceae, Plumbaginaceae, Lamiaceae, Arecaceae, Scrophulariaceae, Verbenaceae, Celastraceae, Avicenniaceae, Caesalpiniaceae, Rubiaceae, and Proteaceae. A wide range of pharmacological activities have been observed for lapachol and its semi-synthetic derivatives in the literature, such as antileishmanial, anticarcinomic, anti-inflammatory, antimalarial, antiseptic, antitumor, antiviral, bactericidal, fungicidal, insectifugal, pesticidal, schistosomicidal, termiticidal, and viricidal effects. The aim of this review is to discuss in detail the phytochemical properties and pharmacological effects of the title compound that have been reported thus far, highlighting its potential therapeutic benefits for the future. © 2013 Springer Science+Business Media., SCOPUS: re.j, SCOPUS: re.j, info:eu-repo/semantics/published

As a continuation of our ongoing studies aimed to depict the effects and mechanism of action of naturally occurring oxyprenylated phenylpropanoids and polyketides, in this paper we describe the synthesis and in vitro anti-proliferative effects of selected compounds belonging to the above cited classes of secondary metabolites on six cancer cell lines using the MTT colorimetric assay. Our study revealed that among the natural products tested, only oxyprenylated chalcones exhibited an appreciable effect (mean IC50 = 32 - 64 ?M), while substituted alcohols, phenylpropenes, naphthoquinones, and aminoacid derivatives were by far less active or inactive., SCOPUS: ar.j, info:eu-repo/semantics/published

As a continuation of our ongoing studies aimed to depict the effects and mechanism of action of naturally occurring oxyprenylated phenylpropanoids and polyketides, in this paper we describe the synthesis and in vitro anti-proliferative effects of selected compounds belonging to the above cited classes of secondary metabolites on six cancer cell lines using the MTT colorimetric assay. Our study revealed that among the natural products tested, only oxyprenylated chalcones exhibited an appreciable effect (mean IC50 = 32 - 64 ?M), while substituted alcohols, phenylpropenes, naphthoquinones, and aminoacid derivatives were by far less active or inactive., SCOPUS: ar.j, info:eu-repo/semantics/published

info:eu-repo/semantics/published

info:eu-repo/semantics/published