共查询到20条相似文献,搜索用时 10 毫秒
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Graziella CappellettiDaniele Cartelli Bruno PerettoMicol Ventura Marco RiccioliFrancesco Colombo John S. SnaithStella Borrelli Daniele Passarella 《Tetrahedron》2011,67(38):7354-7357
The use of tubulin as a target to influence the composition of the mixture from a dynamic combinatorial library, based on the disulfide bond exchange reaction, is described. ESI-FT-ICR-MS was used to determine the composition of the library. The heterodimeric compound amplified by this approach was used to design the homologous derivative with a two-carbon spacer in place of the disulfide function. The ability of the compounds to inhibit tubulin polymerization is reported and compared to thiocolchicine. 相似文献
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Dr. A. Gastón Orrillo Dr. Andrea M. Escalante Prof. Dr. Ricardo L. E. Furlan 《Chemistry (Weinheim an der Bergstrasse, Germany)》2016,22(20):6746-6749
Reversibility of dithioacetal bond formation is reported under acidic mild conditions. Its utility for dynamic combinatorial chemistry was explored by combining it with orthogonal disulfide exchange. In such a setup, thiols are positioned at the intersection of both chemistries, constituting a connecting node between temporally separated networks. 相似文献
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Mlynarski J Rakiel B Stodulski M Suszczyńska A Frelek J 《Chemistry (Weinheim an der Bergstrasse, Germany)》2006,12(31):8158-8167
The asymmetric aldol-Tishchenko reaction of aromatic aldehydes with aliphatic and aromatic ketones has been developed as an efficient strategy for the synthesis of anti-1,3-diols in good yield with high diastereocontrol and good levels of enantioselectivity. This domino-type reaction is catalyzed by a chiral ytterbium complex that promotes both the aldol reaction through enolization of the carbonyl compound and the Evans-Tishchenko reduction of the aldol intermediate. The stereochemistry of the resulting diols is also investigated and finally proved by using CD techniques. 相似文献
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This paper describes the generation of a dynamic combinatorial library of sialic acid analogues using sialic acid aldolase. Addition of wheat germ agglutinin to the equilibrating libraries results in selective amplification of one or more members. 相似文献
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A dynamic library of 15 mono- and bi-conjugated oligonucleotides was generated from a pool of three aldehydes and an oligonucleotide bearing two reactive amino groups. Addition of complementary target to the equilibrating mixture of imines resulted in selective amplification of one conjugate. UV-melting experiments confirmed that it was the best ligand among those that were tested. This study emphasizes that dynamic combinatorial chemistry can be used to simultaneously identify the type and the location of appended residues for stabilizing oligonucleotide complexes. 相似文献
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The constitutional recomposition of a dynamic library of imines displays a complex behavior under the effect of two parameters, acidity and temperature. A qualitative analysis of the quantitative data is presented. The results illustrate the response of such a dynamic system to a physical stimulus (temperature) and a chemical effector (H+), thus demonstrating its adaptive behavior under the pressure of external factors. They also point to the possibility of modulating a given functional property (optical, electronic, ionic) by constitutional recomposition induced by a specific trigger. Such features are of great interest for the development of stimuli-responsive, functional dynamic materials. 相似文献
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Milanesi L Hunter CA Sedelnikova SE Waltho JP 《Chemistry (Weinheim an der Bergstrasse, Germany)》2006,12(4):1081-1087
A well known strategy to prepare high affinity ligands for a biological receptor is to link together low affinity ligands. DCC (dynamic combinatorial chemistry) was used to select bifunctional protein ligands with high affinity relative to the corresponding monofunctional ligands. Thiol to disulfide linkage generated a small dynamic library of bifunctional ligands in the presence of calmodulin, a protein with two independently mobile domains. The binding constant of the bifunctional ligand (disulfide) most amplified by the presence of calmodulin is nearly two orders of magnitude higher than that of the corresponding monofunctional ligand (thiol). 相似文献
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Hiroko Inoue 《Tetrahedron》2008,64(3):493-499
Chiral bis(oxazolinyl)phenyl-rhodium complexes act as catalysts in the combination of AgOTf for direct aldol reaction of ketones and aromatic aldehydes to give the corresponding β-hydroxyketones in high anti-selectivity and a good to high enantioselectivity up to 91% ee. 相似文献
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《Angewandte Chemie (International ed. in English)》2017,56(9):2503-2507
The C‐branched sugar d ‐apiose (Api) is essential for plant cell‐wall development. An enzyme‐catalyzed decarboxylation/pyranoside ring‐contraction reaction leads from UDP‐α‐d ‐glucuronic acid (UDP‐GlcA) to the Api precursor UDP‐α‐d ‐apiose (UDP‐Api). We examined the mechanism of UDP‐Api/UDP‐α‐d ‐xylose synthase (UAXS) with site‐selectively 2H‐labeled and deoxygenated substrates. The analogue UDP‐2‐deoxy‐GlcA, which prevents C‐2/C‐3 aldol cleavage as the plausible initiating step of pyranoside‐to‐furanoside conversion, did not give the corresponding Api product. Kinetic isotope effects (KIEs) support an UAXS mechanism in which substrate oxidation by enzyme‐NAD+ and retro‐aldol sugar ring‐opening occur coupled in a single rate‐limiting step leading to decarboxylation. Rearrangement and ring‐contracting aldol addition in an open‐chain intermediate then give the UDP‐Api aldehyde, which is intercepted via reduction by enzyme‐NADH. 相似文献