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Peter Spenst Prof. Dr. Frank Würthner 《Angewandte Chemie (International ed. in English)》2015,54(35):10165-10168
A rigid, covalently linked perylene‐3,4:9,10‐tetracarboxylic acid bisimide (PBI) cyclophane was synthesized by imidization of a bay‐substituted perylene bisanhydride with p‐xylylenediamine. The interchromophoric distance of approximately 6.5 Å establishes an ideal rigid cavity for the encapsulation of large aromatic compounds such as perylene and anthracene with binding constants up to 4.6×104 M ?1 (in CHCl3). For electron‐poor guest molecules, the complexation process is accompanied by a significantly increased fluorescence, whereas the emission intensity is dramatically quenched by more electron‐rich guests because of the formation of charge‐transfer complexes. Furthermore, the influence of the PBI core twist on the binding constant results in a remarkable selectivity towards more flexible aromatic guest molecules. 相似文献
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Drug innovation is not only reflected in the discovery of new chemotypes of active compounds against existing targets but also more dependent on the innovation of drug targets. Currently, a number of attractive and validated targets could not be targeted pharmacologically. Some have been described as “undruggable”. In this review, we summarized the current situation of “undruggable” targets, and the design strategies for “undruggable” targets, hoping to provide references for the development of innovative drugs. 相似文献
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A “Distorted‐BODIPY”‐Based Fluorescent Probe for Imaging of Cellular Viscosity in Live Cells
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Hao Zhu Dr. Jiangli Fan Miao Li Jianfang Cao Dr. Jingyun Wang Prof. Dr. Xiaojun Peng 《Chemistry (Weinheim an der Bergstrasse, Germany)》2014,20(16):4691-4696
Cellular viscosity is a critical factor in governing diffusion‐mediated cellular processes and is linked to a number of diseases and pathologies. Fluorescent molecular rotors (FMRs) have recently been developed to determine viscosity in solutions or biological fluid. Herein, we report a “distorted‐BODIPY”‐based probe BV‐1 for cellular viscosity, which is different from the conventional “pure rotors”. In BV‐1 , the internal steric hindrance between the meso‐CHO group and the 1,7‐dimethyl group forced the boron–dipyrrin framework to be distorted, which mainly caused nonradiative deactivation in low‐viscosity environment. BV‐1 gave high sensitivity (x=0.62) together with stringent selectivity to viscosity, thus enabling viscosity mapping in live cells. Significantly, the increase of cytoplasmic viscosity during apoptosis was observed by BV‐1 in real time. 相似文献
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M.L. Zheludkevich A.G. Gusakov A.G. Voropaev E.N. Kozyrski S.A. Raspopov A.A. Vecher 《Journal of membrane science》2008,320(1-2):528-532
Permeation of atomic as well as molecular hydrogen through palladium membranes has been investigated experimentally in the temperature range from room temperature to 200 °C and at a higher incident flux of hydrogen atoms on palladium surface than in previous studies. The results demonstrate that phenomena of ‘superpermeability’ and ‘pumping’ of atomic gases through metal membranes are of a common nature. A theoretical model based on chemical thermodynamics and diffusion theory adequately describes the quantitative relationships observed in experiments. It was found that permeability of atomic hydrogen depends strongly on the magnitude of surface incident flux and membrane temperature. 相似文献
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Sebastian Vollbrecht Guergana Dobreva Ioana Cartis Wolf‐W. du Mont Jrg Jeske Frank Ruthe Peter G. Jones Ludger Ernst Walter Grahn Ulrich Papke Michael Marzini Hermann A. Mayer 《无机化学与普通化学杂志》2008,634(8):1321-1325
Oxidative coupling of racemic 1‐ethoxy‐1‐oxophosphindolin‐3‐one ( 1 ) and its 5‐CF3‐derivative 6 with SeO2 furnishes 1,1′‐diphosphaindigo derivatives 5 and 7 as bis‐phosphinic esters, i. e. as PV‐compounds. Like indigo and thioindigo, 5 and 7 exist in the E‐configuration; the crude products of 5 and 7 are mixtures of isomers that are trans‐ and cis‐configurated with respect to the relative orientation of the ester groups oat phosphorus. The structure of the centrosymmetric E‐P(R)P′(S) isomer [(E)‐trans‐isomer] of 5 was determined by X‐ray crystallography. Ester cleavage of 5 , followed by addition of triethylamine to bis‐phosphinic acid 9 (the 1,1,1′,1′‐tetroxide of “phosphoindigo”), furnishes the related bis‐triethylammonium salt 10 as a crystalline hydrate that exhibits an extended hydrogen bonding network. 相似文献
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“Head‐to‐Middle” and “Head‐to‐Tail” cis‐Prenyl Transferases: Structure of Isosesquilavandulyl Diphosphate Synthase
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Jian Gao Dr. Tzu‐Ping Ko Lu Chen Dr. Satish R. Malwal Jianan Zhang Xiangying Hu Fiona Qu Dr. Weidong Liu Dr. Jian‐Wen Huang Dr. Ya‐Shan Cheng Dr. Chun‐Chi Chen Yunyun Yang Prof. Dr. Yonghui Zhang Prof. Dr. Eric Oldfield Prof. Dr. Rey‐Ting Guo 《Angewandte Chemie (International ed. in English)》2018,57(3):683-687
We report the first X‐ray crystallographic structure of the “head‐to‐middle” prenyltransferase, isosesquilavandulyl diphosphate synthase, involved in biosynthesis of the merochlorin class of antibiotics. The protein adopts the ζ or cis‐prenyl transferase fold but remarkably, unlike tuberculosinol adenosine synthase and other cis‐prenyl transferases (e.g. cis‐farnesyl, decaprenyl, undecaprenyl diphosphate synthases), the large, hydrophobic side chain does not occupy a central hydrophobic tunnel. Instead, it occupies a surface pocket oriented at 90° to the hydrophobic tunnel. Product chain‐length control is achieved by squeezing out the ligand from the conventional allylic S1 binding site, with proton abstraction being achieved using a diphosphate‐Asn‐Ser relay. The structures revise and unify our thinking as to the mechanism of action of many other prenyl transferases and may also be of use in engineering new merochlorin‐class antibiotics. 相似文献
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Teresa Kowalska 《Microchemical Journal》1984,30(3):418-424
An attempt was undertaken to furnish an entirely quantitative characteristics to the thermodynamic model of the chromatographic system presented in (2). The attempt proved to be successful and one managed to establish simultaneously a new method enabling direct determination of the hydrogen-bond enthalpy from the PC experimental results. 相似文献
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The properties of polymer alloys are strongly dependent on their phase morphologies. Usually, the phase dispersion and domain sizes are affected by the process and can be influenced and stabilized only “extrinsically” by dispersants and emulsifiers. But, there are some examples of alloys with phase morphologies which are “intrinsically” determined and thus independently of the processing conditions. This aspect of phase determining factors is discussed using four principally different examples of polymer alloys. 相似文献
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