Thiophene bioconjugates with methionine or tryptophan methyl esters have been prepared by reaction of chlorocarbonyl thiophene with the corresponding amino acid ester in the presence of NEt3. The coordination behaviour of these new ligands towards Ag(I) and Au(I)/Au(III) complexes has been studi...

1,2-Bis(sulfonyl)hydrazine derivatives, designed to generate several of the electrophilic species classically believed to be responsible for the alkylating (chloroethylating) and/or carbamoylating activities of the chloroethylnitrosoureas (CNUs), were compared with respect to the cross-linking a...

1,2-Bis(methylsulfonyl)-1-(2-chloroethyl)-2-[[1-(4-nitrophenyl)ethoxy]carbonyl]hydrazine (KS119) is a prodrug of the 1,2-bis(sulfonyl)hydrazine class of antineoplastic agents designed to exploit the oxygen-deficient regions of cancerous tissue. Thus, under reductive conditions in hypoxic cells t...

In this paper we report the synthetic procedures providing the C-substitution of the cobalt bis(dicarbollide) sandwich anion [(1,2-C2B9H11)-3,3′-Co]− with primary, secondary and tertiary alkylamine groups of different length of the aliphatic spacer attached to the carbon C(1) or C(1) and C(1′)...

A novel class of experimental fungicides has been discovered, which consists of special N-thiazol-4-yl-salicylamides. They originated from amide reversion of lead structures from the patent literature and are highly active against important phytopathogens, such as Phytophthora infestans (potato ...

The 6b gene (AK-6b) of Agrobacterium tumefaciens AKE10 can substitute for the requirement of tobacco tissues for auxin and cytokinin to maintain callus growth in the culture medium. To identify compounds that might be involved in this process we analyzed phenolic metabolites in transgenic tobacc...

Assessing the health of marine mammal sentinel species is crucial to understanding the impacts of environmental perturbations on marine ecosystems and human health. In Arctic regions, beluga whales, Delphinapterus leucas, are upper level predators that may serve as a sentinel species, potentiall...

UBV photometry of the W UMa type eclipsing binary AK Her is presented. Light curves analysis were carried out using W–D code to obtain physical parameters of both components. The updated O–C diagram analysis yielded the values of Pmod1=62.61±0.01 years, Pmod2=25.05±0.01 years and Pmod3=13.91...

The manuscript deals with the design, synthesis and biological evaluation of novel benzoxazinone-based and indole-based compounds as multifunctional neuroprotective agents. These compounds inhibit human adenosine kinase (hAK) and human glycogen synthase kinase 3 beta (hGSK-3β) enzymes. Computat...

In E. coli, a single oligomeric enzyme transcribes the genomic DNA, while multiple auxiliary proteins and regulatory RNA interact with the core RNA polymerase (RP) during different stages of the transcription cycle to influence its function. In this work, using fast protein isolation techniques ...

Three novel mononuclear complexes, [MⅡ(L)2·2H2O], (M = Cu, Ni or Cd; HL = 4-(3,4-dichlorophenyl)piperazine-1-carboxylic acid)were synthesized and structurally determined by single-crystal X-ray diffraction. Molecular docking study preliminarily revealed that complex 1 had potential urease inhi...

The present study was undertaken to assess and compare the in vitro cytotoxicity of toxins T-514 and T-544 of buckthorn (Karwinskia humboldtiana) using primary cultures of rat hepatocytes and keratinocytes. Cell cultures were exposed to 6, 12, 25 and 50 μM toxins for 2-, 4-, 6- and 24-h peroids...

Toxin T-514 is a dimeric anthracenone isolated from the Karwinskia humboldtiana (buckthorn) plant. Its potential anti-neoplastic effect was evaluated in vitro and the results obtained were compared with the effect of other known anti-cancer agents. Normal and malignant continuous cell lines were...

T-514 (Peroxisomicine A1) from Karwinskia humboldtiana is a dimeric hydroxyanthracenone with a highly selective cytotoxic effect on tumor cells. We evaluated the metabolism of this compound in two in vitro systems (liver microsomes and hepatocytes) and assessed the cytotoxicity of its metabolite...

In the present study we have analyzed the production of reactive oxygen species by toxin T-514 of the genus Karwinskia in vitro (primary liver cell cultures and microsomes), as well as their possible role in its cytotoxicity. The role of catalase and superoxide dismutase (SOD) as defense mechani...

Karwinskia parvifolia possesses the highest concentration levels of the anthracenone T-514 (PA1). Studies have demonstrated the induction of apoptosis by PA1 in cancer cell lines. The aim was to investigate the effects of PA1 on the apoptosis of the mouse liver in vivo and its underlying pathway...

The previously reported6, unequivocal synthesis of the title compound (5a) afforded a general method for the preparation of 4-substituted 4-thiazoline-2-thiones derived from fully acetylated α-halo ketoses. Such use of the α-halo ketoses (1b) or (2b) (as outlined in MethodI of the Scheme) led ...

Publisher SummaryThis chapter discusses 2-(aldo-polyhydroxyalkyl)benzimidazoles and substances of this type containing hydroxylated side chains of one to seven carbon atoms in length. Typical is the benzimidazole from D-glucose through D-gluconic acid. The side chain is attached at position 2 of...

2-Substituted thiazolidine-4(R)-carboxylic acids (TD) were found to increase the concentration of non-protein sulphydryls (NPSH) and the activity of rhodanese (thiosulphate sulphurtransferase, EC 2.8.1.1) and 3-mercaptopyruvate sulphurtransferase (EC 2.8.1.2) in mouse liver. These properties sug...

The structure of 4-(d-arabino-tetrahydroxybutyl)-4-thiazoline-2-thione (1) was determined by means of synthesis, and was in agreement with the recent structural assignment by Jochims . Procedures of carbohydrate chemistry afforded typical derivatives of 1, and provided a total synthesis from d-g...