A reverse phase HPLC method based on ion-pair formation was set up for the simultaneous determination of gemcitabine and its metabolite 2′,2′-difluoro-2′-deoxyuridine (dFdU) in plasma samples obtained from cancer patients. The separation was performed on a μBondapack C18 (300 mm × 3.9 mm i....

ABSTRACTGemcitabine (2′,2′-difluoro-2′-deoxycytidine, dFdC) and metabolite (2′,2′-difluoro-2′-deoxyuridine, dFdU) quantification is warranted for individualized treatment strategies. Analyte stability is crucial for the validity of such quantification. We therefore studied the impact of th...

2′,2′-Difluoro-2′-deoxycytidine (dFdC, gemcitabine) is a cytidine analogue active against several solid tumor types, such as ovarian, pancreatic and non-small cell lung cancer. The compound has a complex mechanism of action. Because of the structural similarity of one metabolite of dFdC, dFdU...

To improve the properties of rechargeable lithium ion batteries, like conductivity, SEI-formation, thermal and electrochemical stability, low and high temperature performance and safety new electrolyte salts, novel solvents (co-solvents) and additives have been synthesized. All new anions, solve...

Alkaline phosphatase was solubilized from human and rat tissues usinf papain in the presence of TRITON X-100 and subjected to isoelectric focusing (IEF) in polyacrylamide or agarose gels. Up till now, usually 1- and 2-naphthylphosphates have been used as substrates in order to specifically stain...

Agelasine and agelasimine derivatives with substantially less complicated terpenoid side chains compared to the naturally occurring compounds have been synthesized and their ability to inhibit growth of microorganisms and cancer cells has been studied. Compounds with excellent activity against c...

The first racemic syntheses of agelasimines-A and -B, adenine-related bicyclic diterpenoids from the marine sponge Agelas mauritiana, have been accomplished by means of routes through the diol 10 as a key intermediate for their common diterpene portion. As a result, their structures and relative...

The first total syntheses of (+)-agelasimine-A and (+)-agelasimine-B, adenine-related bicyclic diterpenoids isolated from the marine sponge Agelas mauritiana, have been achieved via a highly stereoselective route. On the basis of the present results, the absolute configurations of both alkaloids...

Docking of randomly selected compounds from the chemical universe database GDB-11, which contains all organic molecules up to 11 atoms of C, N, O, F possible under consideration of simple chemical stability and synthetic feasibility rules, into the NMDA receptor glycine site (1pb7.pdb) lead to t...

A practical and environmentally friendly synthesis of 3-aminomethyl-N-tosyl-indazoles is developed. The in situ formed vinyl azines are reacted with amines to furnish amino functionalized anti-hydrazones in excellent yields. Subsequent copper-catalyzed cyclization at ambient temperature is effec...

Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists with greater selectivity over hERG were identified. SAR studies addressing two distinct alternatives for structural modifications leading to improve hERG selectivity are described.

A series of new 3-aminomethyl-4,11-dihydroxynaphtho[2,3-f]indole-5,10-diones 6–13 bearing the cyclic diamine in the position 3 of the indole ring was synthesized. The majority of new compounds demonstrated a superior cytotoxicity than doxorubicin against a panel of mammalian tumor cells with de...

A series of 2-aminomethyl piperidines has been discovered as novel urotensin-II receptor antagonists. The synthesis, initial structure-activity relationships, and optimization of the initial hit that resulted in the identification of potent, cross-species active, and functional urotensin-II rece...

2-Aminoethanol was used to successively replace hydrazine in the preparation of aminomethyl polystyrene resin thereby facilitating purification and by-product removal. The syntheses of the polypeptides ACP (65–74) and oxytocin demonstrated that the use of aminomethyl polystyrene resin prepared ...

A series of novel aminomethyl-piperidones were designed and evaluated as potential DPP-IV inhibitors. Optimized analogue 12v ((4S,5S)-5-(aminomethyl)-1-(2-(benzo[d][1,3]dioxol-5-yl)ethyl)-4-(2,5-difluorophenyl)piperidin-2-one) showed excellent in vitro potency and selectivity for DPP-IV over oth...

The reactivity of buta-2,3-dienoates towards aziridines is reported. Typically, allenoates react as the 2π-component in the [3+2] cycloaddition with azomethine ylides generated from aziridines, affording 4-methylenepyrrolidines in a site-, regio- and stereoselective fashion. However, N-cyclohex...

An efficient and benign method for the preparation of aminomethyl-substituted fullerenes has been developed. The process, involving catalyst free, visible-light irradiation of 10% EtOH-toluene solutions containing fullerene C60 and N-trimethylsilylmethyl-substituted amines by using a 20 W compac...

A new class of oxazolidinone antibacterials incorporating oxygen-, nitrogen-, or sulfur-containing heterobicyclic C-rings is described. The in vitro potency and in vivo efficacy of these conformationally constrained oxazolidinone analogs are discussed.

A number of gatifloxacin analogues containing a nitroaryl-1,3,4-thiadiazole moiety attached to the piperazine ring at C-7 position were prepared and evaluated as antibacterial agents against a panel of Gram-positive and Gram-negative bacteria. Among synthesized compounds, nitrofuran analog 6a ex...

The purpose of the study is to screen the interactions of fourth generation fluoroquinolone–gatifloxacin with efflux pumps, i.e., P-gp, MRP2 and BCRP. Mechanism of gatifloxacin interaction with efflux transporters may explain its acquired resistance. Such clarification may lead to the developme...