IntroductionO-(2-[18F]Fluoroethyl)-L-tyrosine ([18F]FET) is an established radiotracer used for oncology investigations by Positron Emission Tomography (PET). Main limitations to its widespread use are the synthesis itself (time; cost; radiochemical yield; complexity) and a troublesome and time-...

Supramolecular side-chain liquid crystalline poly(acrylate)s have been prepared by self-assembly of H-bond donor and acceptor complexes through intermolecular complementary hydrogen bond formation. Poly[4-(m-acryloyloxyalkyloxy)benzoic acid]s [m = 6 (P1) and 8 (P2)] were employed as polymer comp...

Four macrolides—6-O-methyl-8a-aza-8a-homoerythromycin, clarithromycin, azithromycin and azithromycin 11,12-cyclic carbonate, have been selected for the construction of a series of new quinolone derivatives. The quinolone moiety is connected to the macrolide scaffold via a diaminoaklyl 4″-O-pro...

A set of novel macrolones containing the flexible C8 basic linker and quinolone 3-(2′-hydroxyethyl)carboxamido group has been prepared and structurally characterized by NMR and IR spectroscopy, mass spectrometry and molecular modeling. The new compounds were evaluated in vitro against a panel o...

Following the withdrawal of novobiocin, the introduction of a new ATPase inhibitor of DNA gyrase to the clinic would add the first representative of this mechanistic class to the antibacterial pipeline. This would be of great importance because of the well-known problems associated with antibact...

The synthesis of novel bis-thione ligand, bis(1-benzyl-imidazole-2-thione)methane, SSBn is reported for the first time. This ligand along with the previously reported bis(1-methyl-imidazole-2-thione)methane, SSMe has been utilised in the synthesis of a series of copper(I) halide complexes. The s...

Dietary garlic has been suggested to possess anticancer properties, and several attempts have been made to isolate the anticancer compounds. In this study, we efficiently synthesized N-benzyl-N-methyl-dodecan-1-amine (BMDA) by the reductive amination method. We evaluated the potential anticancer...

Tin(IV) complexes of formulae, [Sn(acpysme)(C6H5)2Cl], [Sn(acpysbz)(C6H5)2Cl], [Sn(acpysbz)(C6H5)Cl2] and [Sn(acpysbz)I3] (acpysme and acpysbz = anionic forms of the 2-acetylpyrazine Schiff bases of S-methyldithiocarbazate and S-benzyldithiocarbazate, respectively) have been synthesized and stru...

UIO-66-NH2[email protected] has been synthesized by anchoring a molecular nickel furfural (Fu) complex into a functionalized nanoporous metal-organic framework (MOF) with the amine functional groups, using the one-pot post-synthetic modification. This new catalyst was identified via Fourier-tran...

The 9-cis and 11-cis stereoisomers of 13,14-dihydroretinoic acid with S configuration, (S)-7 and (S)-9, respectively, have been synthesized stereoselectively. The former has been recently characterized as the first endogenous natural ligand of the retinoid X receptor (RXR). The Julia-Kocienski r...

The goal of this study was to investigate the potential use of a radioiodinated benzamide, N-[2-(1′-piperidinyl)ethyl]-3-iodo[125I]-4-methoxybenzamide (P[125I]MBA), a sigma receptor binding radioligand for imaging breast cancer. The chemical and radiochemical syntheses of PIMBA are described. T...

4-[123I]Iodo-N-{2-[4-(6-trifluoromethyl-2-pyridinyl)-1-piperazinyl]ethyl}benzamide (1.123I), a potential SPECT 5-HT1A radioligand, was evaluated in vivo in rats. Biodistribution studies were performed leading to a % ID in the brain of 0.22 at 5 min p.i. No significant differences in % ID/g tissu...

4-(4-Fluorobenzoyl)-1-[2-(4-iodo-2,5-dimethoxyphenyl)ethyl]piperidine (7) and its derivatives modified at the carbonyl group of the fluorobenzoyl moiety were prepared and evaluated for affinity at 5-HT2A, 5-HT2C (rat cortex) and 5-HT2B (rat stomach fundus) serotonin receptors. Compound 7 bound t...

Reaction of trans-2-methyl-6-oxabicyclo[3.2.1]octan-7-one with trimethylsilyl iodide, generated in situ, followed by refluxing with ethanol gives regioselectively ethyl cis-(and trans-) 5-iodo-2-methylcyclohexane-1-carboxylate, a persistent attractant for male Mediterranean fruit flies.

Ethyl (1R, 2R, 5R)-5-iodo-2-methylcyclohexane-1-carboxylate is a potent attractant for the Mediterranean fruit fly. This compound was stereoselectively synthesized on a multigram scale in nine steps in 15% yield. Key steps of the synthesis involved an asymmetric Diels–Alder reaction, iodolacton...

Both racemic ethyl 5-iodo-2-methylcyclohexanecarboxylate (1), known as Mediterranean fruit fly attractant ceralure B1, and its (−)-(1R,2R,5R) enantiomer 1a were conveniently synthesized from commercially available racemic trans-6-methyl-3-cyclohexenecarboxylic acid 2 or its (1R,6R) enantiomer 2a...

This work reports the synthesis, radiolabeling and preliminary in vitro evaluation of [131I]-5-iodo-N-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinoline-2-yl)-ethyl]-2-methoxy-benzamide. The tributylstannylprecursor was synthesized with a yield of 38%. Radiolabeling was performed using an electrophil...

Methyl caffeate is a natural ingredient with several biological activities, but its preparation is generally limited to chemical synthesis. To set up a simple, high-yield and low-cost synthesis process for obtaining methyl caffeate, a novel synthesis method using the lipase-catalyzed esterificat...

The objective of this study was to investigate the anticancer activity of caffeate derivatives in human cancer cells. Our results demonstrate that caffeate derivatives decreased the population growth of COLO 205, assessed using the MTT assay. However, caffeate derivatives, at the concentrations ...

Phytosterols and their derivatives are relevant in food, pharmaceuticals, and cosmetics. In addition to their well-known effect in lowering low-density lipoprotein (LDL) cholesterol, they also possess other biological activities, such as anti-inflammatory, anti-atherogenicity, and anti-carcinoge...