This objective of this study was to investigate the toxicogenomics and the spatial regulation of global gene expression profiles elicited by endoplasmic reticulum (ER) stress inducer tunicamycin (TM) in mouse small intestine and liver as well as to identify TM-modulated nuclear factor-E2-related...

Publisher SummaryThis chapter discusses the inhibition of dynamic protein palmitoylation in intact cells with tunicamycin (TM). Biological roles of protein palmitoylation are investigated principally through mutational analysis of individual protein substrates. The only documented inhibitor of p...

Aneural cultures of Xenopus myocytes were treated with cycloheximide or tunicamycin in order to determine the influence of continued protein synthesis and insertion of glycosylated acetylcholine (ACh) receptor proteins on developmental changes in ACh-activated single-channel events. The developm...

2-(3-(Naphthalen-2-yl)propanamido)cyclohex-1-enecarboxylic acid and its 6-hydroxynaphthalen-2-yl analogue are well-known hydroxyl-carboxylic acid (HCA) receptor HCA2 agonists. A series of novel aryl derivatives of 2-amidocyclohex-1-ene carboxylic acid that contained rigidity elements, such as an...

Metal-free facile synthesis of pyrano[4,3-b]quinoline-1-ones is described from methyl 2-arylethynylquinoline-3-carboxylates via intramolecular cyclization in excellent yields. The cyclization reactions are facilitated using cheap and easily available KOH base in MeOH. The reaction conditions did...

The addition of mono- and dianions of ethyl N-pivaloyl-3-aminocrotonate to substituted nitroarenes, followed by action of silylating or acylating agent, leads to 3-aminoquinoline carboxylic acid derivatives. Hydrolysis and decarboxylation of the latter, carried out efficiently under relatively m...

An efficient synthesis of methyl ketones from terminal olefins using PdCl2/CrO3 system mimicking the Wacker process is developed. The method shows good functional groups compatibility, no aldehyde by-products and is operationally simple. CrO3 is the sole oxidant and replaces both Cu-salts and mo...

Developmental Toxicity of Amesergide Administered by Gavage to CD Rats and New Zealand White Rabbits. Kelich, S. L., Meade, P. L., II, and Seyler, D. E. (1995). Fundam. Appl. Toxicol. 27, 247-251.Amesergide is a selective serotonin 5-HT1C/2 receptor antagonist being developed for the treatment o...

Amesergide, a serotonin (5-HT2) antagonist intended to treat depression, was administered orally to female CD rats (20/group) at doses of 0, 3, 10, or 30 mg/kg to evaluate effects of mating, fertility, litter size, live birth index (100 × total liveborn progeny/litter size), progeny survival, a...

The dimeric cyclometallated derivatives of palladium(II) [(L-H)PdCl]2, 3 (L = 1, Diazepam: 7-chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one) and 4 (L = 2, Prazepam: 7-chloro-1-cyclopropylmethyl-1,3-dihydro-5-phenyl-2H-1,4-benzodiazepin-2-one) react with triphenylphosphine to giv...

The B-cell lymphoma-2 (Bcl-2) family proteins are attractive targets for cancer therapy. In our previous work, the structure-activity relationship of WL-276 was studied. According to the results, rhodanine derivatives show potent binding affinity for Bcl-2 and Mcl-1 protein and show weaker activ...

α-Oxy/thio substituted-β-keto esters were synthesized through an efficient cross-Claisen condensation of aryl oxy/thio acetic acid ethyl esters with acid chlorides, then it is converted in situ into 4-oxy/thio substituted-1H-pyrazol-5(4H)-ones by the addition of hydrazine or hydrazine derivati...

Both c-Met and VEGFR-2 were important targets for cancer therapies. In order to develop reversible and non-covalent c-Met and VEGFR-2 dual inhibitors, a series of [1,4]dioxino[2,3-f]quinazoline derivatives were designed and synthesized. The enzyme assay demonstrated that most target compounds ha...

The polymerization of p-chloromethyl styrene was conducted by using metallic cationic initiators generated electrochemically. The molecular weight of the polymer obtained by using V, Ti, Cr, Al and Hg was in the range 1000–4000. The effect of type of metallic initiator and the anion of the supp...

Conductivities were measured at 298.15 K for LiClO4, LiAsF6, Bu4NCl, Bu4NClO4, Bu4NBPh4 and Ph4AsCl in 2-(chloromethyl)tetrahydrofuran, and for LiAsF6 in tetrahydrofuran. Comparing these results with literature data for THF and 2-methyltetrahydrofuran systems, it is found that the nature of the ...

Publisher SummaryAlthough the early efforts to extend the chloromethyl ketones series to arginine derivatives met with chemical difficulties, two active site directed inhibitors of trypsin and trypsinlike enzymes are now available: Nα-p-nitrobenzyloxycarbonyl-L-arginine chloromethyl ketone (p-N...

Dilithiation of 2-(chloromethyl)-3-tosylpropene (1) with n-butyllithium at −90°C in the presence of DMPU affords the allylic dianion 2 which reacts with deuterium oxide or very reactive alkylating agents to give α,α-disubstituted products 3 or 4, respectively. Monoalkylation at the α-positio...

A new ligand, 4-chloromethyl-2-(2-hydroxybenzilidenehydrazino) thiazole, has been synthesized from dicholoroacetone and 2-hydroxybenzylidenethiosemicarbazon. Metal complexes of the ligand were prepared from acetate salts of Co(II), Cu(II), Ni(II) and chloride of Cr(III) in dry acetone. Character...

Oligo (styrene-co-chloromethyl styrene) with a molecular weight range of between 1 × 103 and 4 × 103 g mol-1 reacts with potassium 2, 6-di-tert-butylphenoxide salt in dimethyl formamide (DMF) to form polymeric antioxidants. The functionality of such antioxidants was determined by titrating the...

The reactivities of 1-chloro-3-p-tolylsulfinyl acetone (RS)-1 towards diazomethane and of the resulting diastereoisomeric 1-chloromethyl-1-sulfinylmethyl oxiranes 2 towards O-, N- and C-centred nucleophiles are investigated. The synthesis of differently functionalized homochiral chlorinated sulp...