Within a series of histamine H3-antagonists characterized by a biphenyl core and two basic groups, we identified (S)-1-{[4′-((2-methylpyrrolidin-1-yl)methyl)biphenyl-4-yl]methyl}piperidine as a lead scaffold to introduce an additional lipophilic chain at the benzylic carbon close to the pyrroli...
The synthesis and structure–activity relationships of a series of simple biphenyls is described. Optimization of the 4-hydroxy-biphenyl template led to compounds with ERβ selectivity on the order of 20–70-fold.
The combination of antagonism at histamine H3 receptors and inhibition of acetylcholinesterase has been recently proposed as an approach to devise putative new therapeutic agents for cognitive diseases. The 4,4′-biphenyl fragment has been reported by us as a rigid scaffold leading to potent and...
Five new fluorescent macrocyclic ligands derived from biphenyl are described. These new compounds can be used in cation and anion recognition and sensing. Their fluorescent and electrochemical properties are studied and the influence of the biphenyl conformation on these properties is considered...
Twenty-six unsymmetrical biphenyls were synthesized and evaluated for cytotoxic activity against DU145, A549, KB and KB-Vin tumor cell lines. Three compounds 27, 35 and 40 showed very potent activity against the HTCL panel with an IC50 value range of 0.04–3.23 μM. In addition, fourteen active ...
A panel of three lipid-modified, functionalized biphenyl cross-linkers (fBph) were synthesized and subsequently employed in the preparation of the stapled oxyntomodulin (OXM) analogs. In a luciferase-based reporter assay, these stapled OXM analogs showed varying degree of potency in activating G...
The clastogenic potential of 4CMB was assessed in vitro in human lymphocytes from 4 donors (2 male and 2 female) both with and without auxiliary metabolic activation. Although there were some variation in the response of the cells from different donors to 4CMB using 2 criteria for interpretation...
4-Chloromethylbiphenyl (4CMB), benzyl chloride (BC) and 4-hydroxymethyl-biphenyl (4HMB) were tested for biological activity in the following assays: (i) the Salmonella/microsome assay; (ii) a bacterial ‘fluctuation’ assays; (iii) a DNA repair assay in Hela cells, and (iv) a mouse lymphoma muta...
Benzyl chloride (BC) and 4-chloromethylbiphenyl (4CMB) induce a class of alkaline-stable DNA damage in human cells which, like UV-induced pyrimidine dimers, undergoes repair at a slow rate by an excision-repair pathway which can be inhibited by cytosine arabinoside (araC). In the present study, ...
Both benzyl chloride and 4-chloromethylbiphenyl induce repairable types of DNA damage in cultured human cells. No DNA damage can be detected after treatment with 4-hydroxymethylbiphenyl.
Treatment of Syrian hamster embryo cells with 4-chloromethylbiphenyl produced reproducible and quantitative concentration-dependent enhancement of viral transformation the statistical significance of which was independent of cell lethality. These results suggest this compound has carcinogenic po...
The mutagenic activity of 4-chloromethylbiphenyl was determined in Salmonella typhimurium strains TA1535, TA1537, TA98, and TA100 using the plate-incorporation assay with and without rat-liver S9. The compound was positive in strains TA1537, TA98, and TA100 both with and without S9 activation. A...
4-Chloromethylbiphenyl (4CMB) was tested in mice in a dominant lethal assay over 4 weeks. Ethyl methanesulphonate (EMS) was used as the positive control. 4CMB did not elicit a dominant lethal response though EMS produced the expected result.
Six unsymmetrical bis-quaternary monooximes viz. dibromides of 1-(4-hydroxyiminomethyl pyridinium)-3-(3/4-carbamoyl pyridinium)propane, 1-(4-hydroxyiminomethyl pyridinium)-4-(3/4-carbamoyl pyridinium) butane, 1-(4-hydroxyiminomethyl pyridinium)-5-(3/4-carbamoyl pyridinium)pentane were synthesize...
4,4′-Bis(methylene)biphenylene bridged homodinuclear titanocene (3) and zirconocene (4) have been synthesized by treatment of CpTiCl3 and CpZrCl3 · DME with Na2[C5H4CH2C6H4-p-C6H4CH2C5H4], respectively, in THF and characterized by 1H NMR and element analysis. After activation with methyl alumi...
The superfine interaction constants of the cation-radicals of some silicoorganic polyviologens which have not previously been described show that the dimethylsilyl groups play only a small part in the spin density distribution. The interaction of poly-N,N′-1,3-bis-(methylene)tetramethyldisiloxy...
Photocycloaddition reactions of 6,6′-dimethyl-4,4′-[bis(methylenoxy)phenylene]-di-2-pyrones (4a–c) with benzophenone (2a) by mixing in the solid state (solid solution) afforded the corresponding oxetane derivatives (5a–c; 1:2 adducts) with high site- and regioselectivity across the C5–C6 an...
Copolycondensations of 3,3-bis(chloromethyl)oxetane with various diphenols under phase transfer conditions have been performed. The copolyethers show mesomorphism; investigations of their LC properties by optical polarization microscopy and DSC analyses were carried out.
As described in this article, 4,4′-bis(chloromethyl)biphenyl was obtained in 85% excellent yield by chloromethylation of biphenyl catalyzed by the recyclable temperature-dependant phase-separation system that comprised the dicationic acidic ionic liquid PEG1000-DAIL and methylcyclohexane under ...
Malaxinic acid (MA) is a phenolic acid compound, found mainly in pear fruits (Pyrus pyrifolia N.), that is isoprenylated on the C-3 position of benzoic acid. Recently, the effects of prenylated phenolics on health have received much interest owing to their reported potent beneficial biological e...
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