Pyrolysis of the 3-O-allyl derivative 7 of isovanillin followed by alkylation of the derived allylphenol 8 afforded a series of benzaldehyde derivatives 9–11 each of which was transformed by initial treatment with methylmagnesium bromide followed by oxidation of the corresponding alcohols with ...

The compound 7,12-dimethylbenz[a]anthracene (DMBA), a powerful chemical carcinogen, undergoes enzymatic oxidation to a variety of metabolites. Phenols, the monohydroxylated derivatives of DMBA, are an electrophilic species capable of binding covalently with DNA. Although phenols may play a role ...

Benz[a]anthracenes are ubiquitous environmental carcinogens that exert estrogenic and antiestrogenic effects directly or via hydroxylated metabolities. In this paper, the structure-estrogen receptor binding relationships of four, 3,9-benz[a]anthracene diols are described: unsubstituted, 7-methyl...

Centchroman is a non-steroidal oral contraceptive and has been found to be a candidate drug for breast cancer exhibiting partial to complete remission of lesions in 40.5% of breast cancer patients. The therapeutic efficacy of centchroman was monitored alone and together with glycine soya on grow...

Due to limited treatment options for advanced-stage metastatic breast cancer, a high priority should be given to develop non-toxic chemopreventive drugs. The value of various natural and dietary agents to reduce the risk of developing breast cancer is well established. Trianthema portulacastrum ...

Earlier studies from this laboratory of the metabolism of 7,12-dimethylbenz[a]anthracene (DMBA) and of benzo[a]pyrene as well as studies of mutagenic and carcinogenic activity of some of the metabolic products led to the concept that a necessary first step in carcinogenesis by most alkyl substit...

Aim of the present study was to investigate the chemopreventive potential of ferulic acid on 7,12-dimethylbenz[a]anthracene (DMBA) induced mammary carcinogenesis in Sprague–Dawley rats. The chemopreventive potential of ferulic acid was assessed by monitoring the tumor incidence, as well as anal...

The synthesis of novel push–pull 2,4-disubstituted quinazolines was performed by the bromodeoxygenation of 2-phenyl-, 2-(fluoren-2-yl)- and 2-cymantrenylquinazolin-4-ones and subsequent palladium-catalyzed Suzuki reactions. According to the optical studies, derivatives containing 4-positioned 4...

A new magenta-to-transmissive electrochromic polymer, poly(3,4-bis(3-bromopropoxy)thiophene) (PBBrPOT) was synthesized by electrochemical polymerization and its electrochromic properties were characterized in detail. Compared with the representative “large-volume alkyl substituents” strategy, ...

The effect of 1-(3-phenoxypropyl) pyridazin-1-ium bromide, a new pyridazinium derivative, on steel corrosion in a HCl (1 M) solution was analyzed using electrochemical impedance and XPS spectroscopy. Experimental results indicated that the inhibition efficiency increased with an increase in an i...

It is known that acids and bases when mixed together have the potential to react, however, there is complexity when materials are in the solid state, as the surface of the solids may not have all functional groups of the molecule expressed in equal proportions. Conceptually a drug that is acidic...

Cefditoren is a third-generation cephalosporin developed by Meiji Seika Kaisha Ltd. Many β-lactam antibiotics are transported by the H+/peptide symporters PEPT1 and PEPT2 that are preferentially expressed in the luminal membrane of the intestine and kidney, respectively. In this study, we emplo...

AimCefditoren Pivoxil hydrogel tablets were prepared to achieve the gastro retentive effect in order to improve its absorption and bioavailability.

Electrochemical behavior of cefditoren pivoxil (CTP) was studied via experimental electrochemical methods and theoretical calculations performed at B3LYP/6-31+G(d)//AM1 level. Experimental studies were carried out based on an irreversible 4e−/4H+ reduction peak at ca. −0.8 V on hanging mercury d...

Summary :Cefditoren, a third génération cephalosporin antibiotics, has been used in clinics extensively. Previous results have indicated that cefditoren is excreted into bile as unchanged form. To investigate whether canalicular membrane transporters of hepatocytes were involved in the biliary...

Superporous gastro-retentive cefditoren pivoxil tablets were prepared to improve the absorption and bioavailability of this drug and evaluated by varying the concentrations of carbopol and sodium carboxymethyl cellulose. The pre-compression and post-compression parameters were within acceptable ...

Oral antibiotic therapy for patients with acute exacerbations of chronic obstructive pulmonary disease (COPD) usually involves an aminopenicillin with clavulanic acid, a macrolide, or a quinolone. To date, however, the clinical efficacy and safety of the oral cephalosporin cefditoren pivoxil has...

Norfloxacin (NOR) in milk may influence mammalian cell replication and bring about a decrease in the efficiency for treating infection in humans. However, current techniques for detecting NOR usually require expensive instruments and trained personnel. In this work, we have developed a low-cost ...

In the present work, Ti mesh loaded with Ag “nanobosk” was prepared through electro-deposition and characterized with X-ray diffraction, scanning electron microscopy and X-ray photoelectron spectroscopy. Then, the surface enhanced Raman scattering of norfloxacin on the Ti mesh loaded with Ag “...

Nanosponges are a novel class of hyperbranched cyclodextrin-based nanostructures that exhibits remarkable potential as a drug host system for the improvement in biopharmaceutical properties. This work aims the development of cyclodextrin-based nanosponge of norfloxacin to improve its physicochem...