Molecules, Volume 13, Issue 2

Oral delivery is the most common and preferred route of drug administrationalthough the digestive tract exhibits several obstacles to drug delivery including motilityand intraluminal pH profiles. The gut milieu represents the largest mucosal surfacee...

The effects of anonaine, an aporphine isoquinoline alkaloid, on dopaminebiosynthesis and L-DOPA-induced cytotoxicity in PC12 cells were investigated. Anonaineat concentration ranges of 0.01-0.2 μM showed a significant inhibition of dopaminecontent at...

The first guaian-12-oic acid glucopyranosyl ester was isolated from the roots ofPicris rhagadioloides (L.) Desf. (Asteraceae), in addition to five costuslactone-typeguaianolides, four germacranolides and three phenolic compounds. This is the first ti...

Most cancer therapeutics (chemo, radiation, antibody-based, anti-angiogenic)are at best partially and/or temporarily effective. In general, the causes for failure can besummarized as: (i) poor diffusion and/or nonuniform distribution of drug/prodrugm...

Euphorbia wallichii of the family Euphorbiaceae yielded a new rearrangedpentacyclic triterpene of the multiflorane class which we have named spirowallichiione.The structure of this natural spirocompound was elucidated with the aid of modernspectrosco...

Mammalian carboxylesterases (CESs) comprise a multigene family whose geneproducts play important roles in biotransformation of ester- or amide-type prodrugs. Theyare members of an α,β-hydrolase-fold family and are found in various mammals. It has bee...

This paper describes an efficient synthesis and the antiparasitic evaluation ofcyclic β-amino acid-containing dipeptides 3.1-3.6 and 4.1-4.5. The antimalarial propertiesof all these dipeptides have been evaluated in vitro against Plasmodium falciparu...

1,1-Dimethyl-3-oxo-1,4-diazepan-1-ium chloride (1) and 1,1-dimethyl-1-carboxymethyl-3-aminopropyl ammonium hydrochloride (2) have been obtained by thereactions of 1,1-dimethyl-1,3-propylenediamine with ethyl chloroacetate and chloroaceticacid, respec...

The compound L-valine-3-{8-[(E)-2-[3-methoxyphenyl)ethenyl]-7-methyl-1-propargylxanthine-3-yl}propyl ester hydrochloride (MSX-4) was synthesized as an aminoacid ester prodrug of the adenosine A2A receptor antagonist MSX-2. It was found to bestable in...

Paclitaxel (1a), a well known antitumor agent adopted mainly for the treatmentof breast and ovarian cancer, suffers from significant disadvantages such as low solubility,certain toxicity and specific drug-resistance of some tumor cells. To overcome t...

The synthesis of a set of 1-aryl-2-aryl(3-pyridyl)ethanones 1-5 and thecorresponding ketoximes 6-9 is reported. Structural studies of oximes 6, 7 and 9 wereperformed in solution using ¹H-NMR and in the solid state by X-ray crystallography,providing e...

Nitroalkanes can be profitably employed as carbanionic precursors for theassembly of dihydroxy ketone frameworks, suitable for the preparation of spiroketals. Thecarbon-carbon bond formation is carried out exploiting nitroaldol and Michael reactions,...

2-Acetylcyclopentanone undergoes a smooth reaction with triphenylphosphineand dialkyl acetylenedicarboxylates to produce dialkyl 2-(1-acetyl-2-oxocyclopentyl)-3-(1,1,1-triphenyl-λ⁵-phosphanylidene)succinates. These compounds undergo intramolecularWit...

A simple and efficient protocol has been developed for the Michael addition ofamines to α,β-unsaturated esters under microwave irradiation. Under these conditions therewas a significant decrease in the reaction time, increases in the yields and incre...

Rutaecarpine is an indolopyridoquinazolinone alkaloid isolated from Evodiarutaecarpa and related herbs, which has shown a variety of intriguing biological propertiessuch as anti-thrombotic, anticancer, anti-inflammatory and analgesic, anti-obesity an...

Three new compounds: 2R,3R-pterosin L 3-O-β-D-glucopyranoside (1), β-Dxylopyranosyl(1→2)-7-O-benzoyl-β-D-glucopyranoside (2) and 4-O-benzoyl-β-D-xylopyranosyl(1→2)-7-O-benzoyl-β-D-glucopyranoside (3), together with nine knowncompounds, were isolated...

Two new compounds, 6′-O-caffeoyl-p-hydroxyacetophenone-4-O-β-D-glucopyranoside(1) and 6-amino-9-[1-(3,4-dihydroxyphenyl)ethyl]-9H-purine (2) wereisolated from the aerial parts of Artemisia capillaris Thunb. The structures wereestablished on the basis...

Cholesterylbutyrate (Chol-but) was chosen as a prodrug of butyric acid.Butyrate is not often used in vivo because its half-life is very short and therefore too largeamounts of the drug would be necessary for its efficacy. In the last few years butyri...

p-Nitrophenyl acetate is the most commonly used substrate for detecting thecatalytic activity of esterases, including those that activate prodrugs in human cells. Thissubstrate is unstable in aqueous solution, limiting its utility. Here, a stable chr...

The new diterpene methoxy-ent-8(14)-pimarenely-15-one (1) and three knownmetabolites: ent-8(14)-pimarene-15R,16-diol (2), stigmasterol (3) and β-sitosterol (4), wereisolated from the roots of the mangrove plant Ceriops tagal. Their structures and rel...

We have previously shown that ethanol or chloroform extracts of the leaves ofImpatiens balsamina (LIB) have anti-tumor activity against the human hepatocellularcarcinoma cell line HepG2. The ethanol extracts were separated into five fractionsaccordin...