Tubulin is the target of many anticancer drugs, including N-phenyl-N′-(2-chloroethyl)urea (CEU). Unlike most anti-β-tubulin agents, CEUs are protein monoalkylating agents binding through their N′-(2-chloroethyl)urea moiety to an amino acid nearby the colchicine-binding site on β-tubulin isof...

1-Methyl-4-phenylpyridinium ion, a major brain metabolite of the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine, is an inhibitor of Complex I of the mitochondrial respiratory chain. We have synthesized several analogs of 1-methyl-4-phenylpyridinium ion containing various alkyl groups in...

A new family of phenstatin analogues has been synthesized and assayed. This family simultaneously incorporates modifications of the A-ring (replacement of the 3,4,5-trimethoxyphenyl by the 2,3,4-trimethoxyphenyl arrangement), B-ring (N-alkyl-5-indolyl) and conversion of the Oxygen keto group int...

The four fragments A-D previously prepared for the synthesis of amphoteronolide B have been assembled to provide the titled compound. This assembly represents a formal synthesis of amphoteronolide B.

SummaryMost polyene macrolide antibiotics are glycosylated with mycosamine (3,6-dideoxy-3-aminomannose). In the amphotericin B producer, Streptomyces nodosus, mycosamine biosynthesis begins with AmphDIII-catalyzed conversion of GDP-mannose to GDP-4-keto-6-deoxymannose. This is converted to GDP-3...

ObjectiveSynthesize a new BPA-free monomer for use in methacrylate-based materials and evaluate critical properties of resin and composite materials based on the monomer.

2-Cyclohexenones containing an electron withdrawing group in the 4-position and the corresponding N-alkyl-1,3-cyclohexadien-1-amines undergo regioselective iodination and aromatization to give 2-iodophenols and N-alkyl-2-iodoanilines, respectively, upon reaction with iodine and sodium alkoxide. ...

A novel and highly efficient heterogeneous gold(I)-catalyzed [2 + 2 + 2] annulation between ynamides and nitriles has been developed that proceeds smoothly under mild conditions and provides a general and powerful tool for the preparation of a variety of tetrasubstituted pyrimidines with high at...

A new efficient synthesis of isoquinoline-1,3(2H,4H)-diones or isoindolin-1-ones via sequential Ugi-4CR or Ugi-3CR/cyclization reaction was developed. α-Acylamino amides 5, obtained from Ugi-4CR of methyl 2-formylbenzoate, amines, isocyanates and acids, cyclized to give isoquinoline-1,3(2H,4H)-...

Potential antimicrobial activities of azabicyclic skeleton based N-cyclohexyl-2-(2,4-diphenyl-3-azabicyclo[3.3.1]nonan-9-ylidene)hydrazinecarbothioamides (6–10) was synthesized. The newly synthesized compounds were characterized by FT-IR, 1H NMR, 13C NMR, HRMS and elemental analysis. The synthe...

Inexpensive and readily available squamides derived from 9-amino-9-deoxyepiquinine or 9-amino-9-deoxyepiquinidine were found to be superior catalysts for the asymmetric conjugate additions of t-butyl nitroacetate to β,γ-unsaturated-α-ketoesters. After the subsequent decarboxylation with silic...

Five triphenylamine derivatives containing cyclohexyl have been designed and synthesized with a solvent-free green procedure. The compounds possess high quantum yields both in solution and solid state. Our investigation shows that the steric effects of the chair conformation cyclohexyl and stron...

A straightforward stereoselective route towards (3aR,5R,6S,7R,7aR)- and (3aR,5R,6S,7R,7aR)-octahydro-1H-indole-5,6,7-triol, analogues of castanospermine, starting from the corresponding shikimic acid derivatives is described. The key transformations of this approach are the Overman rearrangement...

BackgroundMivacurium is a non-depolarizing muscle relaxant and widely used as a short-acting anesthetic. Pseudo-allergic reactions to mivacurium occur when it is administered during perioperative anesthesia. These reactions may present a serious threat to the patient’s life, particularly in chi...

5-[2-(N,N-diethylamino)ethoxy]-4,7-dimethylcoumarin (1) and 6-acetyl-5-[2-(N,N-diethylamino)ethoxy]-4,7-dimethylcoumarin (2) were synthesized in a traditional way and microwave-assisted synthesis. Crystals of 2 in form of hydrochloride salt (3) were investigated using single crystal X-ray diffra...

A simple and expedient method for the preparation of the ubiquitous 2-(N,N-diethlamino)ethyl aryl ether moiety using a conventional microwave oven has been developed. The reactions are performed with pulsed microwave irradiation, to produce gram quantities of ethers in good yields.

After a preliminary search of the reaction conditions for the Suzuki–Miyaura cross-coupling of haloazulenes with arylboronic acids, the title compounds were synthesized either by the direct coupling reaction between 1,3-dihaloazulene and the corresponding N,N-disubstituted 4-aminophenylboronic ...

Bis-(4-aminophenyl)-sulfone and several N,N'-diacyl derivatives have shown appreciable activity as antimalarials. With the assumption that a molecule more readily cleaved to a p-aminophenyl sulfur or oxidized sulfur anion, as a potential anti-PAB substance, might be a more effective antimal...

Two new analogues of a popular host material, meta-bis(N-carbazolyl)phenylene (mCP), bearing either methoxy- (mCP-OMe) or tert-butyl (mCP-t-Bu) substituents at C-3 and C-6 positions of carbazole moieties were synthesized and characterized. These materials exhibit higher glass-transition temperat...

In this paper, we have synthesized aniline oligomer composite material using heteropolyacid (H4SiW12O40) as dopant. The UV–Vis absorption spectra, the photoluminescence and surface photovoltage properties of the composite materials were studied. The band at 572 nm is weakened and even disappear...