A human oxidoreductase (H-37) that is overexpressed in ethacrynic acid-resistant HT29 colon cells (Ciaccio, P. J., Stuart, J.E., and Tew, K.D. (1993) Mol. Pharmacol. 43, 845-853) has been identified as a dihydrodiol dehydrogenase. Translated protein from a dihydrodiol dehydrogenase cDNA isolated from a library prepared from ethacrynic acid-resistant HT29 cell poly(A+) RNA was recognized by anti...

The synthesis and biological evaluation of ten Michael acceptors containing potential proteasome inhibitors are described. Cellular targets of azide containing inhibitors and were assessed in HEK293T and RAW264.7 cells by a two step labeling strategy, followed by biotin-pulldown, affinity purification, on-bead tryptic digestion and LC-MS(2) identification. This strategy appears to be an attract...

Thia-Michael reactions between aliphatic and aromatic thiols various Michael acceptors were performed under environmentally-friendly solvent-free conditions using Amberlyst® A21 as a recyclable heterogeneous catalyst to efficiently obtain the corresponding adducts in high yields. Ethyl acrylate was main acceptor used, although others such acrylamide, linear, cyclic enones also utilized successf...

the studies performed about electrochemical oxidation 2-amino-4-methylphenol indicate that ortho-quinone yielded through oxidation of this chemical compound was unstable and it could be used as michael acceptor under solvent influences, carrier electrolyte, additives and could be transformed into the various compounds in the form of 1-4 addition michael reaction. based on this, in the paper fir...

Heteroarylvinyl sulfone 1 has been successfully used as a new sulfonyl Michael acceptor in aminocatalytic reactions with branched aldehydes. Subsequent one-pot Julia-Kocienski olefination allows the challenging preparation of enantiomerically pure α-allylated aldehydes bearing C-α quaternary carbons.

The aza-Michael addition is a versatile reaction for the modification of ?,?-unsaturated carbonyl compounds with amines. reactivity dimethyl itaconate as bio-based Michael acceptor explored in this work. Through its reactions piperidine and dibutylamine, it was found that order can be changed by choice catalyst, solvent, or concentration amine reactant. effectiveness catalysts proportional to t...

The unusual sugars, α-aculosides, which appear in certain antibiotics and have an α,β-unsaturated ketone structure, were found to be novel and selective Michael acceptors for the thiol function of cysteine residues. A coumarin derivative possessing α-aculoside as a Michael acceptor effectively and irreversibly operated as a fluorescent probe in cells. Furthermore, α-aculosides exhibited cytotox...

A highly enantio- and diastereoselective intramolecular Stetter reaction has been developed. Subjection of alpha,alpha-disubstituted Michael acceptors to an asymmetric intramolecular Stetter reaction results in a highly enantioselective conjugate addition and a diastereoselective proton transfer. Available evidence suggests the diastereoselective protonation occurs via intramolecular delivery t...

An optimisation of Michael-type addition of azole derivatives of broad-scale acidity - ranging from 5.20 to 15.00 pK(a) units - namely 4-nitropyrazole, 3,5-dimethyl-4-nitropyrazole, 4(5)-nitroimidazole, 4,5-diphenylimidazole, 4,5-dicyanoimidazole, 2-methyl-4(5)-nitroimidazole, 5(4)-bromo-2-methyl-4(5)-nitroimidazole and 3-nitro-1,2,4-triazole to methyl acrylate as an acceptor was carried out. T...

The studies performed about electrochemical oxidation 2-amino-4-methylphenol indicate that ortho-quinone yielded through oxidation of this chemical compound was unstable and it could be used as Michael acceptor under solvent influences, carrier electrolyte, additives and could be transformed into the various compounds in the form of 1-4 addition Michael reaction. Based on this, in the paper fir...