A new series of estrogen receptor modulators: effect of alkyl substituents on receptor-binding affinity

New types of selective estrogen receptor modulators (SERMs) were synthesized and evaluated for their binding affinity and biological effect on reproductive cells. A proposed lead structure (B) was derivatized to provide compounds 30 and 44, which showed good estrogen-receptor binding affinity (K(i) values: 6.3 and 10 nM, respectively), as well as minimal impact on mammary and uterine carcinoma cells. Introduction of an alkyl group in the core structure considerably enhanced receptor-binding affinity of the compounds tested. Synthesis and structure-activity relationships of these compounds are described.     

Conditional Expectations Relative to a Product State and the Corresponding Standard Potentials

For a lattice system with a finite number of Fermions and spins on each lattice point, conditional expectations relative to an even product state (such as Fermion Fock vacuum) are introduced and the corresponding standard potential for any given dynamics, or more generally for any given time derivative (at time 0) of strictly local operators, is defined, with the case of the tracial state previously treated as a special case. The standard potentials of a given time derivative relative to different product states are necessarily different but they are shown to give the same set of equilibrium states, where one can compare states satisfying the variational principle (for translation invariant states) or the local thermodynamical stability or the Gibbs condition, all in terms of the standard potential relative to different even product states.     

Inclusion Behavior of 4-Nonylphenol into Cyclodextrin Derivatives

The solubilities of 4-nonylphenol in five kinds of hydroxypropyl-cyclodextrin (HP-CDs) solutions were investigated in order to evaluate them for soil remediation. The relative aqueous-phase concentration of 4-nonylphenol linearly increased with the increasing HP-CD concentration. The addition of HP-beta-CD (degree of substitution, D.S.=0.6) produced the largest change because the inner core of HP-beta-CD is the most hydrophobic. The solubility of 4-nonylphenol in the HP-CD solutions depended upon the cavity diameter and the degree of HP-CD substitution. Both ozone and activated carbon treatments have been using for removing organic compounds and foul odor compounds from tap water. As the inclusion complexes moved into the groundwater, the ozone degradation of the inclusion complexes was estimated. The 4-nonylphenol-HP-CD inclusion complexes were easily degraded by ozone. The degree of degradation increased with the increasing ozonization time. Weakly acidic compounds were produced from the 4-nonylphenol-HP-CD inclusion complexes by ozonization. HP-CDs could be used for the removal of 4-nonylphenol from soil. Copyright 2001 Academic Press.     

Synthesis of new tricyclic mesoionic amides via photochemical conversion of a 5‐azido‐1‐mesityl‐3‐phenyltetrazolium salt

New mesoionic amides 4 and 5 with novel tricyclic ring systems have been synthesized by the photolysis of a 5‐azido‐1‐mesityl‐3‐phenyltetrazolium salt 1c via the corresponding triplet nitrene inter mediate. The structure of 5 has been determined by X‐ray crystallography.     

Multi-purpose explosion chamber with sound muffling and vibration cutting means

Abstract

An explosion chamber is operating for more than 13 years successfully. The chamber is used for procucing wBN powder and various dynamic high pressure experiments. The capacity of the chamber is 200 cubic meter by volume and 10 kg by the quantity of the explosives to be exploded. Safety means are equipped sequentially, transmitted sound level is less than 65 db at 60 m point from the chamber and earth vibrations cannot be detected at its periphery. The strength of the chamber was designed by simple static gas pressure model.     

Simultaneous evaluation of one‐electron reducing systems and radical reactions in cells by nitroxyl biradical as probe

In the present study, a novel probe for the simultaneous evaluation of one‐electron reducing systems (electron transport chain) and one‐electron oxidizing systems (free radical reactions) in cells by electron chemical detection was developed. Six‐membered cyclic nitroxyl radicals (2,2,6,6‐tetramethylpiperidine‐1‐oxyl; TEMPO series) are sensitive to one‐electron redox systems, generating the hydroxylamine form [TEMPO(H)] via one‐electron reduction, and the secondary amine form [TEMPO(N)] via one‐electron oxidation in the presence of thiols. In contrast, the sensitivities of five‐membered cyclic nitroxyl radicals (2,2,5,5‐tetramethylpyrrolidine‐1‐oxyl; PROXYL series) to the one‐electron redox systems are comparatively low. The electron chemical detector can detect 2,2,6,6‐tetramethylpiperidine‐1‐oxyl (TEMPO), TEMPO(H) and PROXYL but not TEMPO(N). Therefore, nitroxyl biradical, TEMPO‐PROXYL, as a probe for the evaluation of one‐electron redox systems was employed. TEMPO‐PROXYL was synthesized by the conjunction of 4‐amino‐TEMPO with 3‐carboxyl‐PROXYL via the conventional dicyclohexyl carbodiimide reaction. TEMPO‐PROXYL, TEMPO(H)‐PROXYL and TEMPO(N)‐PROXYL were simultaneously quantified by HPLC with Coularray detection. Calibration curves for the quantification of TEMPO‐PROXYL, TEMPO(H)‐PROXYL and TEMPO(N)‐PROXYL were linear in the range from 80 nm to 80 μm , and the lowest quantification limit of each molecule was estimated to be <80 nm . The relative standard deviations at 0.8 and 80 μm were within 10% (n = 5). Copyright © 2015 John Wiley & Sons, Ltd.     

SERS studies of isolated and agglomerated gold nanoparticles functionalized with a dicarboxybipyridine‐trimercaptotriazine‐ruthenium dye

A dicarboxybipyridine‐trimercaptotriazine ruthenium complex, primarily designed for dye solar cells, has been successfully employed for generating electrostatically stabilized gold colloids, because of its high negative charge and capability of binding to gold nanoparticles via the sulfur groups. Surprisingly, a strong surface‐enhanced Raman scattering enhancement has been observed for the isolated nanoparticles, exceeding those recorded after inducing agglomeration. Such unusual response has been ascribed to the predominant contribution of the charge‐transfer and resonance Raman mechanisms, more than compensating for the lack of the local hot spots, in relation to the agglomerated systems. Copyright © 2014 John Wiley & Sons, Ltd.