The reactions of aldrin and photoaldrin with phthaloyl peroxide in carbon tetrachloride provided the respective carbon tetrachloride adducts, epoxides and cyclic phthalates of the corresponding cis-diols.Under the same conditions isodrin yielded the half-cage ketone (14), the cyclic phthalate (1...

Photodieldrin and photoaldrin-two major metabolites of insecticides, dieldrin and aldrin readily undergo stereospecific dehydrohalogenation in the presence of superoxide (O−2) under relatively mild conditions.

Novel 1H-benzo[d]immidazole-4-carboxamide derivatives bearing five-membered or six-membered N-heterocyclic moieties at the 2-position were designed and synthesized as PARP-1 inhibitors. Structure-activity relationships were conducted and led to a number of potent PARP-1 inhibitors having IC50 va...

In order to explore the antiproliferative effect associated with the piperazine framework, several 1-benzhydrylpiperazine derivatives 8(a–d), 9(a–d) and 10(a–h) were synthesized. Variation in the functional group at N-terminal of the piperazine led to three sets of compounds, bearing the sulf...

Two new sulfonated (SDA) and carboxylated (CDA) aromatic diamine-diol monomers were synthesized and applied to prepare thin-film composite (TFC) nanofiltration (NF) membranes with improved antifouling and performance properties. The interfacial polymerization method was used to make sulfonated a...

The oxidation system comprised of TEMPO and (diacetoxyiodo)benzene (stoichiometric) is enhanced during the conversion of primary alcohols to aldehydes by adding a catalytic amount of acids, p-TsOH and PPTS. 2-Alkylidene-1,3-propanediols, available from 1,3-dihydroxyacetone, are oxidized under th...

Three-residue peptides capped with benzyloxycarbonyl (Z-) group, Z-Pro-Leu-Gly–NH2 and Z-Pro-Leu-Gly–OH, are investigated by infrared (IR) spectroscopy, using supersonic-jet laser desorption technique, in the N–H and O–H stretching frequency ranges. The IR spectra show clear evidence of the ...

This paper presents a derivatization, mass fragmentation study relating to the most common six cholic acids, such as cholic, lithocholic, chenodeoxycholic, ursodeoxycholic, 3-hydroxy,7-ketocholanic and dehydrocholic acids, identified and quantified as pollutants in the aquatic environment at the...

4-Cyclohexylbutyl-N-[(S)-2-oxoazetidin-3-yl]carbamate (3b) is a potent, selective and systemically active inhibitor of intracellular NAAA activity, which produces profound anti-inflammatory effects in animal models. In the present work, we describe structure–activity relationship (SAR) studies ...

Two new steroidal esters with an unusual framework, Sinkiangenorin A and B, a new organic acid glycoside, Sinkiangenorin C, and four known lignin compounds were isolated from the seeds of Ferula sinkiangensis. The structures of these compounds were established by spectroscopic analysis and singl...

We synthesized several candidates of 24(S)-hydroxycholesterol (24S-OHC) esters, which are involved in neuronal cell death, through catalysis with acyl-CoA:cholesterol acyltransferase-1 (ACAT-1). We studied the regioselectivity of the acylation of the secondary alcohol at the 3- or 24-position of...

The effect of a leukemia-inducing treatment on early changes in kinetic parameters of murine bone marrow cells were investigated. Mice were treated i.p. one, four and eight times at bi-weekly intervals with 1 mg DMBA. Up to nine weeks after the last injection, CFU-S number, proliferation ability...

7,12-Dimethylbenz[a]anthracene (DMBA) elicits leukemia in Long–Evans rats (LE). This leukemia is mostly erythroblastic and 30% of leukemias have total and partial trisomy of #2 chromosome and the rest have diploid karyotype. The common duplication site is in 2q26–q34 and N-ras gene is located ...

The leukemogens 7,12-dimethylbenz[a]anthracene (DMBA) and 7,8,12-trimethylbenz[a]anthracene (TMBA) bind covalently in vivo to DNA of Long-Evans rats in the hematopoietic organs, spleen and bone marrow, and in the liver, a non-target organ. Both TMBA and DMBA depleted bone marrow cells and both a...

Stereospecific syntheses of the trans-3,4-dihydrodiol metabolites of 9- and 10-fluoro-7,12-dimethylbenz[a]anthracene, -7-methylbenz[a]anthracene, and -12-methylbenz[a]anthracene are described. These dihydrodiols are putative proximate carcinogenic metabolites that undergo activation by the P-450...

7,12-Dimethylbenz(a)anthracene (DMBA) and 7-methoxymethyl-12-methylbenz (a)anthracene (MeO-DMBA) are converted to a number of products during short exposures in aqueous suspension to laboratory illumination. The mixture of products binds to glyceraldehyde-3-phosphate dehydrogenase (GPDH) while i...

Oligomers of prostaglandin B1 inhibited phospholipase A2 extracted from human neutrophils in a dose-dependent manner (IC50 = 5 μM), while the monomer was not inhibitory at concentrations of 10 μM or less. The inhibitory activity of PGB1 oligomers increased with increasing polymer size; PGB dim...

Chemically synthesized dimers, trimers and tetramers of 15-dehydroprostaglandin B1 and 16,16′-dimethyl-15-dehydroprostaglandin B1 facilitate the release of Ca2+ from isolated rat liver mitochondria. The parent monomeric prostaglandins had no significant activity. The rate of release was stimula...

Cyclooxygenase-2 (COX-2) is highly expressed in tumor cells and has been regarded as a hallmarker for cancers, but the excise regulatory mechanism of COX-2 in tumorigenesis remains largely unknown. Here, we pulled down and identified a novel COX-2 regulator, heterogeneous nuclear ribonucleoprote...

Dimeric derivatives of prostaglandin B1 were prepared under alkaline conditions and the structures were determined by NMR spectroscopies.