A series of unsymmetrical 1,2-bis(imino)acenaphthenenickel(II) halides containing N-2,6-dibenzhydryl-4-methoxyphenyl – a single bulky group with adjusted electron donating properties – has been synthesized and characterized. These compounds adopt distorted tetrahedral geometry and their 1H NMR...

After O-methyloximation of the carbonyl functions, the organic acids in serum and urine are extracted by anion-exchange chromatography, transformed into the methyl esters and pre-fractionated by thin-layer chromatography. In one of the four fractions and on the basis of the nitrogen in the O-met...

As a PI3K and mTOR dual inhibitor, N-(2-chloro-5-(2-acetylaminobenzo[d]thiazol-6-yl)pyridin-3-yl)-4-fluorophenylsulfonamide displays toxicity when orally administrated. In the present study, alkylurea moiety replaced the acetamide group in the compound and a series of 1-alkyl-3-(6-(2,3-disubstit...

The methyl 4-(diethoxymethyl)-3-(pyridin-3-yl)isoxazole-5-carboxylate obtained by domino 1,3-dipolar cycloaddition and elimination starting of pyridine-3-nitrile oxide and methyl 4,4-diethoxy-3-p-tolylsulfinylbut-2-enoate is a convenient scaffold for the synthesis of other new highly functionali...

In continuation of our investigation on novel stearoyl-CoA desaturase (SCD) 1 inhibitors, we have already reported on the structural modification of the benzoylpiperidines that led to a series of novel and highly potent spiropiperidine-based SCD1 inhibitors. In this report, we would like to exte...

A novel series of (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives were identified as selective transient receptor potential vanilloid 4 (TRPV4) channel antagonist and showed analgesic effect in Freund’s Complete Adjuvant (FCA) induced mechanical hyperalgesia model in...

Here we report a structure–activity relationship (SAR) study of analogues of 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro-naphthalen-2-ol. Our SAR is focused on introduction of various substitutions in the piperazine ring of the hybrid template. The goal behind this s...

The synthesis, pharmacological evaluation and molecular modelling study of novel naphthalen-2-yl acetate and 1,6-dithia-4,9-diazaspiro [4.4]nonane-3,8-dione derivatives as potential anticonvulsant agents are described. The newly synthesized compounds were characterized by both analytical and spe...

Experimental design methodology (DOE) surpasses traditional (one variable at a time) approach in improving the chromatographic separation performance with minimum effort and resources. Since combination therapy of oral hypoglycemic drugs was generally recommended by Clinical Practice Guidelines ...

Two Schiff base ligands, 4-(((4-ethylphenyl)imino)methyl)phenol (4EMP) and (E)-4-((naphthalen-2-ylimino) methyl) phenol (4NMP) were synthesized by the reaction of 4-hydroxybenzaldehyde with 4-ethylaniline, 4EMP, or naphthalene-2-amine, 4NMP. The compounds were characterized using NMR (1H and 13C...

Single crystal of (E)-1-(4-ethylphenyl)-3-(4-(heptyloxy)phenyl)prop-2-en-1-one (4EPC) was grown in acetonitrile via slow evaporation solution technique. The molecular structure of 4EPC was then confirmed by single crystal X-ray diffraction analysis and the crystal exhibited monoclinic with centr...

For the first time, a pathway for synthesis of 2-(4-chlorophenyl)-2-(4-chloro-3-thiophenol)-1,1-dichloroethene (3-SH-DDE), is presented. The compound is of particular interest as a precursor for synthesis of alkylsulfonyl-DDE containing different alkyl groups to discover structural activity rela...

Several 2-alkoxycarbonyl- and 2-aryloxycarbony-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazines, conceived as thiolysable prodrugs of 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazine, were synthesized and their antineoplastic activity evaluated against the L1210 leukemia in mice. In additio...

3-Di(methylsulfonyl)methylene-pyrrol-2-one and 2-(1-aryl-5-methoxy-2-oxo-2,3-dihydro-1H-3-pyrrolylidene)malononitrile were obtained from 1-aryl-5-methoxypyrrolones. Aziridine and hydroxylamine reacted with pyrrol-2-one to afford 2,7-diazaspiro[4.4]nona-3,6-diene and oxime derivatives, respective...

The dynamics of organohalogen contaminants and their metabolites are best studied over time by analysis of biota at high trophic levels. In this study, time trends, 1971–2001, of bis(4-chlorophenyl) sulfone (BCPS) and of methylsulfonyl-substituted metabolites of PCBs and 4,4′-DDE, were investi...

PI3K/Akt/mTOR and hedgehog (Hh) signalings are two important pathways in breast cancer, which are usually connected with the drug resistance and cancer migration. Many studies indicated that PI3K/Akt/mTOR inhibitors and Hh inhibitors displayed synergistic effects, and the combination of the two ...

The structures of 5-(4-chlorophenyl)-1-{4-(methylsulfonyl)phenyl}-1H-tetrazole (3) and 4-{5-(4-methoxyphenyl)-1H-tetrazol-1-yl}benzenesulfonamide (5) have been determined by X-ray crystallography. Tetrazoles 3 and 5 crystallize in the monoclinic space groups Ia and P21/c, respectively. The cell ...

Anti-apoptotic proteins, such as B-cell lymphoma (Bcl-2) protein, myeloid cell leukemia sequence 1 (Mcl-1) protein, are potential targets for cancer treatment. In the studies, a series of pyrrolidine derivatives were developed as potent Mcl-1 inhibitors. The preliminary biological studies sugges...

A FeCl3-catalyzed multicomponent reaction was developed for the facile synthesis of coumarin-3-carboxylic ester derivatives in a highly atom-economic and environmentally friendly way. Using simple and cheaply available salicylaldehydes, Meldrum's acid and alcohols as the starting materials,...

New temperature sensitive AB, ABA, and BAB amphiphilic block copolymers consisting of hydrophilic poly(ethylene oxide) and hydrophobic poly(ethyl glycidyl carbamate) blocks were synthesized by anionic polymerization followed by chemical modification reactions. The self-association of the block c...