A series of [1,2,3]triazolo[4,5-d]pyrimidine derivatives bearing a hydrazone moiety were designed, synthesized and evaluated for their antiproliferative activity against several cancer cell lines of different origins by MTT assay. Most of the synthesized compounds demonstrated moderate to good a...

The polymer-supported synthetic protocol for preparation of thiazolidinedione-pyrimidine hybrids was developed and applied for rapid and effective synthesis of a library of variously substituted conjugates. Reported synthetic methodology is based on easy accessible building blocks and very simpl...

The cholesterol esterase-catalyzed hydrolysis of the water-soluble substrate p-nitrophenyl butyrate occurs via an acylenzyme mechanism, and is competitively inhibited by boronic acid transition state analog inhibitors. Accordingly, we undertook to dimensionally map the enzyme's active site ...

A number of 5-arylisatin derivatives were synthesized in 5–6 steps from readily available starting materials. Their structures were confirmed by 1H NMR and 13C NMR as well as LC/MS. The cytotoxicity of these novel isatins against human leukemia K562 cells were evaluated by MTT assay in vitro. S...

A new series of substituted-N-(3,4-dimethoxyphenyl)-benzoxazole derivatives 13a–13p was synthesized and evaluated in vitro for their COX (I and II) inhibitory activity, in vivo anti-inflammatory and ulcerogenic potential. Compounds 13d, 13h, 13k, 13l and 13n exhibited significant COX-2 inhibito...

The development of highly efficient and green catalyst for the one-pot synthesis of 5-substituted tetrazole and polyhydroquinoline derivatives is an extremely important and ground challenging area in organic chemistry. In this study, two catalysts were prepared by the immobilization of Ni and Cu...

Synthesis of chalcones (1,3-diarylprop-2-en-1-ones) and 2-pyrazoline derivatives has been an active field of research due to their established pharmacological effects. In this study, a series of chalcones were prepared with methyl aryl ketones and substituted aldehydes in the presence of sodium ...

The enzyme inosine 5′-monophosphate dehydrogenase (IMPDH) catalyzes an essential step in the de novo biosynthesis of guanine nucleotides, and thus regulates the guanine nucleotide pool required for cell proliferation. Of the two isoforms, human IMPDH type 2 (hIMPDH2) is a validated molecular ta...

A highly chemo- and diastereoselective protocol for the cyclopropanation of tertiary allylic amines with Shi’s carbenoid [CF3CO2ZnCH2I] is described. The high levels of diastereoselectivity observed in these reactions may be attributed to chelation of the nitrogen atom to the zinc reagent, whic...

A new route to 6-deoxy-6-fluorosucrose has been developed. The process proceeds in 8 linear steps in 25% overall yield from sucrose. The steps incorporating fluorine and subsequent deprotection are quite rapid, making the procedure useful in the context of 18F-labeling for PET applications.

A facile synthesis of 6′-deoxy-6′-fluorosucrose has been developed. The title compound is available in six linear steps in 44% overall yield from commercially available sucrose. The synthesis involves rapid and convenient fluorination and deprotection conditions. This procedure would be very u...

A novel carbamoylated quinidine based monolith, namely poly(O-9-[2-(methacryloyloxy)-ethylcarbamoyl]-10,11-dihydroquinidine-co-ethylene dimethacrylate (poly(MQD-co-EDMA)), was prepared for the micro-LC enantioseparation of N-derivatized amino acids. The influence of the mobile phase composition,...

In order to obtain satisfactory column permeability, efficiency and selectivity for micro-HPLC, a capillary monolithic column containing O-9-[2-(methacryloyloxy)-ethylcarbamoyl]-10,11-dihydroquinidine (MQD) as chiral selector was re-optimized. The monolithic column was used to successfully enant...

The complete series of regioisomeric dimethoxybenzoyl-N-methylpiperazines were synthesized and evaluated in GC–MS and FTIR studies. The EI mass spectra show fragment ions characteristic of both the dimethoxybenzoyl and the N-methylpiperazine portions of the molecules. These characteristic fragm...

The six regioisomeric 1-pentyl-3-dimethoxybenzoylindoles can be differentiated by a combination of EI-MS and FT-IR spectra. The six regioisomeric 1-n-pentyl-3-(dimethoxybenzoyl)-indoles represent potential designer modifications in the synthetic cannabinoid drug category. The analytical properti...

Inhibition of acetyl-CoA carboxylases has the potential for modulating long chain fatty acid biosynthesis and mitochondrial fatty acid oxidation. Hybridization of weak inhibitors of ACC2 provided a novel, moderately potent but lipophilic series. Optimization led to compounds 33 and 37, which exh...

Conventional polyimide aerogels made from biphenyl-3,3′,4,4′-tetracarboxylic dianydride (BPDA) and 4,4′-oxidianiline (ODA) exhibit poor resistance to moisture and mechanical properties. In this work, a versatile diamine, 2,2′-bis-(trifluoromethyl)-4,4′-diaminobiphenyl (TFMB), is introduced ...

Histone deacetylases (HDACs) are a class of epigenetic modulators with complex functions in histone post-translational modifications and are well known targets for antineoplastic drugs. We have previously developed a series of bisthiazole-based hydroxamic acids as novel potent HDAC inhibitors. I...

A series of processable new aromatic polyamides (PAs) were prepared by the reaction of a new diacid monomer namely, 2,6-bis[3′-trifluoromethyl-4′(4″-carboxyphenoxy)benzyl]pyridine and previously reported four diamines monomers. The synthesized PAs showed high thermal stability (up to 468 °C ...

Benzyl chlorodifluoromethyl ketone, ethyl bromoacetate and zinc afforded ethyl 3-(chlorodifluoromethyl)-3-hydroxy-4-phenylbutanoate in a Reformatsky-type reaction. By successive stages of dehydration to a mixture of but-2-and -3-enoates; simultaneous hydrogenation of the double bond and replacem...