In order to improve the antitumor and/or antiviral activities of existing nucleoside analogs, eight new compounds (9a,b, 14a,b, 15a,b and 16a,b) were designed and synthesized. Halogen atom were incorporated at the 2-position of the purine base to render the amino group at the 6-position less sus...

A direct and convenient metal-free method to prepare sulfonyl amidines in the presence of aqueous tert-butyl hydroperoxide (T-HYDRO) has been developed. Different tertiary and secondary amines were tested for compatibility with the oxidative conditions and could be coupled with sulfonyl azides t...

A series of 1-isopropylsulfonyl-2-amine benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. In general, these derivatives are potent HBV inhibitors (IC50  40). Compounds 5b–e, g, j, and 9a were am...

Recently, more and more concomitant EGFR mutations and ALK rearrangement are observed from the clinic, which still lacks effective single-agent therapy. Starting from ALK inhibitor 14 (TAE684), we have developed a highly potent EGFR/ALK dual kinase inhibitor compound 18 (CHMFL-ALK/EGFR-050), whi...

Anaplastic lymphoma kinase (ALK)-positive cancers have rising morbidity and mortality in recent years, and novel chemotherapeutic drugs with no drug resistance and high activity for treating ALK-positive cancers are needed urgently. In this study, we investigated the anti-cancer effect of 5-chlo...

α-Phenylthio-α,β-alkenones (2), readily available by Pd(II)-catalysed coupling of (E)-1-phenylthio-1-tributylstannylhex-1-ene with the corresponding acid chlorides, have been treated with borane in the presence of phenylglycine- or proline-derived oxazaborolidines to afford 2-phenylthio-2-alk...

2-Nitro-2-phenylthio oxiranes (3), prepared by nucleophilic epoxidation of 1-nitro-1-phenylthio alkenes (1), react with a variety of heteroatomic nucleophiles to give α-substituted S-phenylthio esters (2). Of special note is the efficient reaction of 2-nitro-2-phenylthio oxiranes with boron tri...

A new method for a regioselective introduction of a bis(methoxycarbonyl)-methyl group into the 4-position of the piperidine skeleton was explored, and this method was applied to the preparation of cis- and trans-2,4-disubstituted piperidines starting from 2-piperidinecarboxylic acid. The key ste...

SummaryIn order to further explore the structure—activity relationships of serotonergic 2-aminotetralin derivatives, a total of 12 aryl and heteroaryl substituents have been introduced in the C8-position of 2-(dipropylamino)tetralin. The affinity of the compounds was studied by competition expe...

Twenty-two 3-O-substituted-3′,4′,5′-trimethoxyflavonols have been designed and synthesized for their anti-proliferative activity towards three human prostate cancer cell lines. Our results indicate that most of them are significantly more potent than the parent 3′,4′,5′-trimethoxyflavonol ...

As the physiologic roles for the different classes of aldehyde dehydrogenase (ALDH) enzymes are elucidated, the identification of specific, reversible inhibitors becomes of great pharmacologic interest. Previous structure-function studies identified dialkylamino substituted benzaldehyde compound...

Interfacial area per surfactant molecule values at the air/liquid interface for heterocyclic and dipropylamino derivatives of zwitterionic hexadecylphosphocholine and cationic cetyltrimethylammonium bromide derivatives were calculated from surface tension measurements in NaBr and salt-free aqueo...

A new and efficient synthesis of (+)-cis-8-methoxy-1-methyl-2-(dipropylamino)tetralin, AJ-76, and its monopropyl analog, UH-232, was achieved. Relative stereochemistry was controlled by doubled bond hydrogenation, followed by enantiomeric resolution with quinine to obtain optically pure material...

A concise synthesis of the β-amyloid1–42 aggregation inhibitor (−)-5,8-dihydroxy-3R-methyl-2R-(dipropylamino)-1,2,3,4-tetrahydronaphthalene [(−)-2] has been developed. The key step is a regio- and diastereoselective hydroboration-amination sequence to convert alkene 6 into amine 9. Enantiomeri...

A series of unknown 3-(alkyl(dialkyl)amino)benzofuro[2,3-f]quinazolin-1(2H)-ones 4–17 has been synthesized as new ellipticine analogs, in which the carbazole moiety and the pyridine ring were replaced by a dibenzofuran residue and a pyrimidine ring, respectively. The synthesis of these benzofur...

The inhibitory effects of 2-amino-4-(4-methoxyphenyl)-thiazole (MPT) on mild steel corrosion were evaluated in 0.5 M H2SO4 and 1 M HCl solutions, respectively. From the analysis of potentiodynamic polarization curves and electrochemical impedance spectroscopy, MPT can effectively inhibit the cor...

Four new N-acyl-2,4-bis(4-methoxyphenyl)-3-azabicyclo[3.3.1]nonanes 3–6 have been synthesized. The structural characterization and the conformational preferences of the compounds 3–6 have been carried out using IR, 1D and 2D NMR and Mass spectral data. The NMR spectral data indicates that the ...

A series of 5-substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine derivatives was synthesized and evaluated for their cyclin-dependent kinase (CDK) inhibition activity. The most potent compounds contained various hydroxyalkylamines at the 5 position and possessed...

Reactions of the metal ions (Co(II), UO2(II), Sm(III), Eu(III) and Zn(II)) with the (2-(4-pyridyl)-1,3-benzothiazole (p-PBT) and (2-(4-pyridyl)-1,3-benzothiazole N-oxide (N-O p-PBT) ligands lead to new complexes of the following types: [Co(p-PBT)2(SCN)2] (1), [Co(p-PBT)2(dca)2](MeOH) (2), [(p-PB...

The reactions of a range of aromatic primary amines with pyridine-2-carboxaldehyde were reported, highlighting the effect of the substituents of the amine on the outcomes of the Schiff base reactions. The variant products of the Schiff base reactions were reacted with cis-[PtCl2(DMSO)2], generat...