Gas phase geometries and strain energies (ES) at 298.15 K and 1 atm were calculated using the G4MP2 composite method and various density functional model chemistries for tetracyclo[3.3.3.13,10 .17,10]tridecane (bowlane) and its methylene spacer edge and lip expanded (−CH2−)n(n = 1–4) homologs. ...
The synthesis of (M)-trispiro[3.0.0.3.2.2]tridecane [(M)-4], the first hydrocarbon with a helical primary structure of four-membered rings, is described. Key step is the kinetic resolution of a cyclobutanone through reduction with bakers' yeast. As compared to its analogue of three-membered...
The critical micelle concentration (CMC) of tridecane, tetradecane and hexadecane phosphonic acids and their mono- and disodium salts were determined with a battery of methods. The CMC values for all the studied species follow the general trend of those of the lower homologos of the series. The ...
The treatment for many diseases can be improved by developing more efficient peptide delivery technologies, for example, biodegradable polymers. In this work, photocrosslinked poly(ester anhydride)s based on functionalized poly(ε-caprolactone) oligomers were investigated for their abilities to ...
Purpose: The aim of this study was to investigate the ability of n-alkenyl succinic anhydrides (n-ASAs) to improve the film-forming characteristics of a novel coating polymer, potato starch acetate degree of substitution 2.8 (SA). n-ASAs were also applied to improve the otherwise brittle propert...
A new enzyme catalysed kinetic resolution of cis-4-benzyloxy-2,3-epoxybutanol has been reported. Efficient, scalable separation of the optically active alcohol from its ester derivative has been solved with liquid–liquid and solid–liquid extraction methods using commercial organic solvents and...
The resistance of tumor cells to the cytostatic activity of methylating and chloroethylating anticancer drugs is determined by the level of expression of the DNA repair protein O6-methylguanine-DNA-methyl-transferase (MGMT). The synthesis of labelled 6-benzyloxy-9H-purin-2-ylamine derivatives sh...
When compounds 3a and 3b were subjected to a Mitsunobu reaction with benzoylthymine, the expected substitution products were formed together with the regioisomers corresponding to benzyloxy group migrations.
Cell surface molecule CD44 plays a major role in regulation of cancer stem cells CSCs on both phenotypic and functional level, however chemical inhibition approach of CD44 to targets CSCs is poorly studied. Herein, we report the discovery of certain N′-(2-oxoindolin-3-ylidene)-2-(benzyloxy)benz...
We report the molecular first hyperpolarizability (β) of a series of nonlinear optical (NLO) chromophores comprising amino-benzene with an additional methoxy or benzyloxy group as the donor units, polyene, phenyl-di-vinylene, or thienyl-di-vinylene as the π-electron bridges, and 2-(dicyanometh...
Alpha-aminoisobutyric acid (AIB) labeled with the cyclotron-produced, positron-emitting radionuclide 11C has been synthesized with the label in the alpha-methyl group. Our previously published synthesis of [11C] AIB in the carboxyl position from [11C] HCN requires a rigorous quality assurance pr...
Objective: To determine serum parameters reflective of androgen status in postmenopausal women using two types of hormone replacement therapy (HRT).Design: Randomized, double-blind, prospective 1-year trial of two oral HRT regimens.Setting: University hospital, department of obstetrics and gynec...
Objective: To investigate the incidence of uterine bleeding during 12 months of treatment with 17β-estradiol (E2) 1 mg, unopposed or in combination with three doses of norethindrone acetate.Methods: This study was a prospective, double-masked, randomized, multicenter trial. A total of 1176 heal...
Dissolution of oral contraceptive combination products from six manufacturing firms was studied utilizing the rotating basket method at 100 rpm in 600 mL of 0.1 M HCl and 0.02% sodium lauryl sulfate (SLS). Most of the combination products of norethindrone (NE):ethinyl estradiol (EE) dissolved sa...
The effects of different monophasic combinations of ethinyl estradiol and norethindrone on FSH, LH, sex hormone binding globulin, total testosterone, androstenedione, and dehydroepiandrosterone sulfate levels in non-obese, non-hirsute women were compared. Retrospective analysis of frozen serum f...
There is limited information on the metabolism of levonorgestrel, norethindrone and structurally related contraceptive steroids. Both levonorgestrel and norethindrone undergo extensive reduction of the α,β-unsaturated ketone in ring A. Levonorgestrel also undergoes hydroxylation at carbons 2 a...
Norethisterone (Chemical s Service Registry Number 68-22-4) is a synthetic progestin used as a contraceptive or in the treatment for amenorrhea and endometriosis. It has moderate potential for bioconcentration. The main route of exposure is ingestion of the drug whose metabolites are mostly excr...
BackgroundEtravirine, a non-nucleoside reverse transcriptase inhibitor (NNRTI) active against NNRTI-resistant HIV, is an inducer of CYP3A4 and an inhibitor of CYP2C9/19.
This study examined the cytochrome P450 (CYP) enzyme selectivity of in vitro bioactivation of lynestrenol to norethindrone and the further metabolism of norethindrone. Screening with well-established chemical inhibitors showed that the formation of norethindrone was potently inhibited by CYP3A4 ...
A series of analogs of the potent HIV-1 integrase (HIV IN) inhibitor chicoric acid (CA) was designed with the intention of ameliorating some of the parent natural product’s undesirable properties, in particular its toxicity, instability, and poor membrane permeability. More than 70 analogs were...
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