A series of derivatives of 2,3-dihydro-2-(aryl)-4(1H)-quinazolinone (DHQZ) with known antitumor activity was re-evaluated in the National Cancer Institute cancer cell line screen. Analysis by the COMPARE algorithm suggested that their cytotoxicity derived from interactions with tubulin. Signific...

A novel series of 2-benzyl-1-indanone analogs were investigated as IL-5 inhibitory activity. Among the synthesized compounds, 7-(cyclohexylmethoxy)-2-(4-hydroxybenzyl)-2,3-dihydro-1H-inden-1-one (7s, 100.0% inhibition at 30 μM, IC50 = 4.0 μM), and 7-(cyclohexylmethoxy)-2-(3-hydroxybenzyl)-2,3-...

The title compound, a potential intermediate to protected C-nucleoside analogs related to formycin A, was synthesized via a new route wherein 2,3,5-tri-O-benzyl-1-O-p-nitrophenyl)-d-ribofuranose was converted to 2,5-anhydro-3,4,6-tri-O-benzyl-d-allonic acid, and further transformed into 4-(tert-...

Tri-block poly(lactide)–poly(ethylene glycol)–poly(lactide) (PLA–PEG–PLA) copolymers and related acrylated derivative were synthesized and used to prepare micelles and nanogels for controlled release of naltrexone. The resulting copolymers, micelles and nanogels were characterized by various...

We transformed naltrexone (5) with the morphinan skeleton into mesembrane (4) belonging to the Sceletium alkaloids via key intermediate 6, characterized by a cis-fused hydroindole skeleton with a suspended phenyl ring fixed by an epoxy bridge. We then investigated the binding affinities of 4 and...

A hydrolyzable crosslinker (N,O-dimethacryloylhydroxylamine (MANHOMA)) was synthesized by a modified method and was characterized using 1H-NMR, FTIR, and melting point determination. Naltrexone-loaded nanoparticles were prepared by copolymerization of poly(ethylene glycol)1000 monomethyl ether m...

A series of alkyl, cycloalkyl, aryl, and aralkyl ethers of naltrexone oxime was prepared. The compounds were examined in binding assays for μ, δ and κ opioid receptor affinity. In addition, the, naltrexone oxime ethers were studied in animal models that measure opioid agonist and antagonist a...

Establishment of in vitro-in vivo correlations (IVIVCs) for parenteral polymeric microspheres has been very challenging, due to their complex multiphase release characteristics (which is affected by the nature of the drug) as well as the lack of compendial in vitro release testing methods. Previ...

Anacardic acids are one of natural products found in not only the cashew nut shell oil but also the nut and fruit juice. The present study was conducted to investigate the uncoupling effect of anacardic acids on oxidative phosphorylation of rat liver mitochondria using succinate (plus rotenone) ...

Merulinic acid (heptadecenylresorcinolic acid, resorcinolic acid) is one of the members of resorcinolic lipids, the natural amphiphilic long-chain homologues of orcinol (1,3-dihydroksy-5-methylbenzene). In the present study, membrane properties of merulinic acid were investigated. Merulinic acid...

SummaryThe age-associated deterioration in cellular and organismal functions associates with dysregulation of nutrient-sensing pathways and disabled autophagy. The reactivation of autophagic flux may prevent or ameliorate age-related metabolic dysfunctions. Non-toxic compounds endowed with the c...

Amphipterygium adstringens is a plant traditionally used to treat gingivitis, gastric ulcer and even gastric cancer but the mechanism involved in the regulation of the immune response is not elucidated yet. The 6-pentadecylsalicylic acid (6SA) is the main anacardic acid found in A. adstringens. ...

Anacardic acid (6-pentadecylsalicylic acid, AA), a natural compound isolated from the traditional medicine Amphipterygium adstringens, has been reported to possess antitumor activities. However, its molecular targets have not been thoroughly studied. Here, we report that AA is a potent inducer o...

Copoly(phenylene-imide)s were synthesized by Ni(0)-catalyzed coupling of aromatic dichlorides containing imide structure and 2,5-dichlorobenzophenone. The route offered the flexibility of incorporating different ratios of benzophenone and imide groups in the polymer backbone in a controlled mann...

The synthesis of some new α-phenylcinnamonitriles is reported along with biological results in the areas of chemotherapy, gastrointestinal activity, fertility control, parasitology, and agricultural screening. The compounds showed negative or marginal biological activity in the areas tested.

The reactions between several transition metal oxyanion salts and Na2S2C2(CN)2 and K2S2C6Cl4 are reported. Oxy-metal bis-dithiolene complexes such as [VOS4C4(CN)4]2−,[VO(S2C6Cl4)2]2− and [MoOS4C4−(CN)4]2− have been isolated and are described, and voltammetric evidence for monoanionic species der...

Tetraphosphorous decasulfide reacted with phenoxyethanol, α and β-naphthol, ortho-toluidine, ortho-aminophenol and ortho-phenylenediamine to give aryl esters or amides of dithiophosphoric acids. These were used as ligands in the synthesis of some nickel(II) and cobalt(II and III) complexes. Wi...

This paper reports the synthesis of dinuclear Mo(V) complexes containing the Mo2S42+ core. Complexes are prepared using the starting material (NH4)2Mo2(S2)6·2H2O for which a new high yield preparation is presented. Reaction of Mo2(S2)62− with eight equivalents of the monodentate thiol, PhSH, gi...

In this Study, a pH-sensitive nanoplatform made up of chitosan (Cs) and mesoporous hydroxyapatite (HAP) was synthesized and employed for delivering of adenosine 5′-triphosphate (ATP). The fabricated system was decorated with folic acid (FA), providing both tumor targeting and imaging. The [emai...

A series of novel anthranilic diamides derivatives containing aryl-isoxazoline moiety were designed and synthesized as a part of our ongoing search for potential anticancer agents. Their structures were confirmed by 1H NMR, 13C NMR and ESI-MS analyses. The preliminary assays showed that some of ...