The boron trifluoride-etherate mediated cyclization of 2-arylthio-ketones 1a-h at ambient temperature gave 3-aryl-substituted benzothiophenes 2a-h in excellent yield. None of the rearranged 2-aryl-substituted benzothiophenes were observed.
Benzofuran-2-boronic acid could be used as a fluorescent sensor for the detection of Pd2+ because it was rapidly converted to highly fluorescent derivative after mixing with Pd2+ under basic condition at room temperature. We found that dimerization of benzofuran was occurred to form fluorescent ...
The design, synthesis, and capacity to inhibit HIF prolyl 4-hydroxylases (PHDs) are described for 2-[2-(3-hydroxy-pyridin-2-yl)-thiazol-4-yl]-acetamide analogs. These analogs revealed two kinds of novel scaffolds as PHD2 inhibitors. Synthetic routes were developed for the preparation of their an...
Two new coordination polymers, [Zn(mpba)2]n (1) and [Cd(H2O)(mpba)2]n (2), have been prepared by reactions of M(NO3)2·6H2O (M = Zn for 1, Cd for 2) with an unsymmetric 3-methyl-5-(pyridin-4-yl)benzoic acid (Hmpba) under hydrothermal condition. Both complexes 1 and 2 were characterized by elemen...
Solvothermal reaction of N,N′-Bis[(pyridin-3-yl)methyl]pyridine-2,5-dicarboxamide (L1) as well as Zn(OAc)2 or Co(NO3)2 in methanol gave rise to two new 2D complexes [Zn(L2)2]n (1) and [Co(L2)2]n (2), in which in situ formation of an anionic ligand 5-((pyridin-3-yl)methylcarbamoyl)pyridine-2-car...
African trypanosomes are incapable of purine de novo synthesis. They use salvage pathways to meet their purine requirements. Therefore, purine analogues appear as potential candidates to interfere in trypanosome metabolism. The acyclic adenosine analogue (S)-9-(-3-hydroxy-2-phosphonylmethoxyprop...
The title compound 1,2-di-O-acetyl-5-O-benzoyl-3-deoxy-l-erythro-pentofuranose (5), a useful precursor for the stereospecific synthesis of β-l-nucleoside analogues as potential antiviral agents, has been synthesised by a multi-step reaction sequence from l-xylose with a 38% overall yield. The p...
Novel l-arabinose, l-ribose, 2-deoxy-l-ribose and 2-fluoro-2-deoxy-l-arabinose derivatives were synthesized from readily available l-arabinose. Different synthetic routes to methyl 3,5-di-O-acylated-l-arabino(ribo)furanosides as valued intermediates for the preparation of C-2 functionalized l-pe...
Estrogen (E2) plays a central role in the development and progression of hormone-responsive cancers. Estrogen metabolites exhibit either stimulatory or inhibitory roles on breast and prostate cells. The catechol metabolite 4-hydroxyestradiol (4-OHE2) enhances cell proliferation, while 2-methoxye...
The use of N-salicylidene-4-methyl-o-aminophenol in nickel(II) pivalate chemistry has provided access to structurally and magnetically interesting {NiII6NaI4} and {NiII6} clusters possessing carbonato and methanediolato(-2) ligands, respectively, with novel coordination modes.
In this study, we have shown that methyl-3,5-di-O-caffeoyl-epi-quinate, a naturally occurring compound isolated from Ainsliaea acerifolia, inhibits receptor activator of nuclear factor-κB ligand (RANKL)-induced formation of multinucleated tartrate-resistant acid phosphatase (TRAP)-positive oste...
Seven new 2-cinnamoyl-1,3-indandione (2CID) O-methyl ethers with different substituents (R = –H, –CH3, –OCH3, –N(C6H5)2, –N(CH2CH2CN)2, julolidyl, –N(CH3)2) in 4-position of the cinnamoyl moiety were synthesized. The methylation with dimethylsulfate occurred at the oxygen atom of the exocy...
Phylloquinone is a redox active naphthoquinone involved in electron transport in plants. The function of this reduced form remains unclear due to its instability, which has precluded detection. Herein, a simple method that permits the stabilization of the reduced form of phylloquinone by di-O-me...
Small interfering RNAs (siRNAs) are an active agent to induce gene silencing and they have been studied for becoming a biological and therapeutic tool. Various 2′-O-modified RNAs have been extensively studied to improve the nuclease resistance. However, the 2′-O-modified siRNA activities were ...
MicroRNAs (miRNAs) are a class of small non-coding RNAs that regulated diverse cellular processes including differentiation, proliferation, apoptosis, metabolism and signal transduction pathways. An increasing number of data suggested that miRNA-21 could be identified as diagnostic and therapeut...
We synthesized several DNA oligonucleotides containing one or several 2′-O-methyl-8-methyl guanosine (m8Gm) and demonstrated that these oligonucleotides not only stabilize the Z-DNA with a wide range of sequences under low salt conditions but also possess high thermal stability. Using artificia...
The effect of 2′-O-(N-methylcarbamoyl)ethyl (MCE) modification on splice-switching oligonucleotides (SSO) was systematically evaluated. The incorporation of five MCE nucleotides at the 5′-termini of SSOs effectively improved the splice switching effect. In addition, the incorporation of 2′-O-...
The single enantiomer (1S,2S)-2-benzyl-2,3-dihydro-2-(1H-inden-2-yl)-1H-inden-1-ol (2), has recently been synthesized and isolated from its corresponding diastereoisomer (1). The molecular and crystal structures of this novel compound have been fully analyzed. The relative and absolute configura...
Squaraines containing 2,3-dihydro-1H-perimidine terminal groups have been known since 1993. In the literature two structure types have been described; those involving bonding of the four-membered ring to C-4 and those involving bonding to C-6 of the dihydroperimidine unit.It was found by extensi...
The Parham Cyclization reaction of o-lithiobenzyl chlorides (generated by low temperature halogen-metal exchange of the corresponding o-bromobenzyl chlorides with n-butyllithium) with azodicarboxylate esters provides a new entry to the 2,3-dihydro-1H-indazole-1,2-dicarboxylate ring system in mod...
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