The first in a series of 2 papers on the synthesis of the insect toxin pederin (1) begins with a discussion of syntheses of the ring A fragments (±)-ethyl pederate (2) and (±)-benzoylselenopederic acid (4). A silicon-mediated intramolecular cyclisation of a chloroformate onto an allyl silane (...

Synthesis and biological evaluation of new chrysene derivatives aimed at the development of anticancer agents were carried out.

In this study, novel 3-O-methoxy-4-halo, disubstituted-5,7-dimethoxy chromans with bacterial cell wall degrading potentials were synthesized, characterized and evaluated as DNA gyrase inhibitors and antibacterial agents. Compounds were showed a broad spectrum of antimicrobial activity against bo...

A simple, efficient, and eco-friendly synthetic protocol has been developed for the synthesis of pyranoxanthenes via one pot three-component reaction. This reaction is between aromatic aldehyde, 2,2-dimethylchroman-7-ol and 1,3-cyclohexanedione by using molecular iodine in AcOH as a reaction med...

A concise approach comprising a combination of the Pd- or Ir-catalyzed Tsuji-Trost allylation and olefin dihydroxylation/acid catalyzed lactonization has been developed to construct the central spirolactone core of trigolutes with the requisite functional groups. A large number of analogues of t...

Synthesis of C-5-substituted 1,3-dioxoisoindoline-4-aminoquinolines having amide group as a spacer was developed with an intent to evaluate their antiplasmodial activities. The synthesized dioxoisoindoline-aminoquinolines tethered with β-alanine as a spacer and secondary amine as substituent di...

c-Met/HGF signaling pathway plays an important role in cancer progression, and it was considered to be related to poor prognosis and drug resistance. Based on metabolite profiling of (S)-7-fluoro-6-(1-(6-(1-methyl-1H-pyrazol-4-yl)-1H-imidazo[4,5-b]pyrazin-1-yl)ethyl)quinoline (1), a series of 2-...

Clitocine, a natural biologically active substance isolated from the mushroom Leucopaxillus giganteus, possesses several bioactivities including antitumor. Here, for the first time, we studied the molecular mechanism of clitocine-induced apoptosis in human cervical cancer cells (HeLa). Clitocine...

ABT-737 is a novel anti-apoptotic Bcl-2 family protein inhibitor with high affinity to Bcl-2, Bcl-xl and Bcl-w but relatively low affinity to Mcl-1/A1. Therefore, high level Mcl-1 usually confers human tumor cell resistance to ABT-737. At the present study, we observed that clitocine can induce ...

Reversed-phase high-performance liquid chromatographic methods were developed for separation and identification of the enantiomers of bicyclic β-amino acids: racemic diendo-(1S,2S,3R,4R and 1R,2R,3S,4S) and diexo-(1S,2R,3S,4R and 1R,2S,3R,4S)-3-amino-bicyclo[2.2.1]heptane-2-carboxylic acids and...

Cyclic β-aminohydroxamic acid enantiomer pairs were stereoselectively separated by high-performance liquid chromatography on the recently developed Cinchona alkaloid-based zwitterionic chiral stationary phases Chiralpak ZWIX(+)™, ZWIX(−)™, ZWIX(+A) and ZWIX(−A). The results of variation of the ...

Chronic infections with hepatitis B virus (HBV) and hepatitis C virus (HCV) lead to serious liver diseases worldwide. Co-infection with HBV and HCV is very common and is associated with increased risk of liver pathogenesis, liver cancer, and liver failure. Several 5-substituted 3′-fluoro (or ch...

The effect of analogues of both 2',3'-dideoxy-3'-fluorothymidine (FddThd) [2',3'-dideoxy-3'-fluorouridine (FddUrd), 2',3'-dideoxy-3'-fluoro-5-chlorouridine (FddClUrd), 2',3'-dideoxy-3'-fluoro-5-bromouridine (FddBrUrd) and 2',3'...

3'-Azido-2',3'-dideoxy-5-iodouridine (AzIdUrd) and 3'-azido-2',3'-dideoxy-5-bromouridine (AzBdUrd), previously shown to be potent and selective inhibitors of human immunodeficiency virus replication invitro were minimally toxic to the uninfected human lymphoid cell ...

Agar dilution susceptibility testing of temafloxacin, cefotetan, clindamycin, and ciprofloxacin was performed in 103 genital tract isolates of Bacteroides. The respective minimum inhibitory concentration inhibiting 90% of the strains tested were temafloxacin, 4 μg/ml; cefotetan, 256 μg/ml; cli...

Temafloxacin is a new fluoroquinolone that achieves a high urine concentration and has potent, broad-spectrum antimicrobial activity against most pathogens associated with urinary tract infections. The clinical efficacy and safety of temafloxacin were assessed in adult females with acute, uncomp...

The pharmacokinetics of temafloxacin were assessed in 12 healthy young and 12 healthy elderly volunteers after oral administration of a single 600 mg dose. Groups were balanced with respect to gender distribution. Plasma and urine temafloxacin concentrations were determined using high-performanc...

This article summarizes animal studies conducted to determine the toxic and mutagenic potential of temafloxacin. The four target tissues of potential concern with fluoroquinolone use are the kidney, the eye, the weight-bearing joints of young animals, and the central nervous system. Based on the...

The bactericidal activity of temafloxacin and other fluoroquinolones is attributed to inhibition of bacterial DNA gyrase (topoisomerase II), an enzyme that regulates supercoiling and uncoiling of DNA. Because of this unique bactericidal mechanism of action, resistance to fluoroquinolones is limi...

A number of fluoroquinolones have been shown to interact adversely with theophylline. We studied the influence of coadministration of temafloxacin, a new fluoroquinolone antimicrobial agent, on steady-state theophylline pharmacokinetics. Twelve healthy subjects (8 males, 4 females; average age a...