In the present research paper corticosteroids prodrugs of hydrocortisone acetate (1) have been synthesized, which was isolated from the flowers of Allamanda Violacea. The hydrocortisone acetate (1) was hydrolyzed to hydrocortisone (2) which was subsequently converted to prednisolone (3). Both th...

An effective epimerization of the normal estrone 3-methyl and 3-benzyl ethers by using o-phenylenediamine and AcOH made the possibility for facile entry into the 13α-estrone series. Combination of this synthetic methodology with an isolation step carried out by means of the Girard-P reagent, th...

The conventional etherification uses toxic or hardly degradable alkylating agents. An eco-friendly tandem etherification/aromatization is presented to prepare estrone 3-secondary ethers from easily available dienone 1. Three marketed 3-etherified estrogen drugs were synthesized with the method f...

13α-Estrone derivatives containing various substituents on C-3 and C-17 were synthesized, and evaluated by means of MTT assays for in vitro antiproliferative activity against a panel of human adherent cancer cell lines (HeLa, MCF-7, A2780 and A431). Compounds with N-benzyltriazolylmethoxy moiet...

Heterocyclization of steroids were reported to give biologically active products where ring D modification occured. Estrone (1) was used as a template to develop new heterocyclic compounds. Ring D modification of 1 through its reaction with cyanoacetylhydrazine and elemental sulfur gave the thio...

The stereochemistry of reduction of the steroid 17-ketone group by Raney nickel catalyst modified by tartaric acid depends on the chirality of the tartaric acid, the pH, and the pressure of hydrogenation.

A Liquid Chromatography coupled to tandem mass spectrometry (LC–MS/MS) based method have been developed for the determination of the main estrogen compounds –estrone (E1) and 17β-estradiol (E2)– in human serum. Two isotope dilution mass spectrometry (IDMS) quantification procedures have been...

13α-Estrone and its 3-methyl or benzyl ether were halogenated in ring A with N-bromo- or N-iodosuccinimide or 1,3-dibromo-5,5-dimethylhydantoin as electrophile triggers. The chemo- and regioselectivities of the reactions depended greatly on the nature of the substituent on C-3. Bromination of t...

An expanding body of evidence indicates the possible role of estrane derivatives as useful anticancer agents. The aim of this study was to describe the cytotoxic effects of 63 newly synthetized estrone-16-oxime ethers on human cancer cell lines (cervix carcinoma HeLa, breast carcinoma MCF7 and s...

Methyl ether of racemic estrone, the long-known steroid, crystallizes in the form of a lamellar conglomerate. This form exhibits many properties of the ordinary conglomerates, however it requires special methods for the enantiomer separation due to pseudoracemic composition of the crystals.

A high-strength polyvinyl alcohol (PVA) hydrogel was prepared via a facile photocrosslinked polymerization with cellulose nanofibrils (CNF) reinforcement. The mechanism of CNF reinforcement was studied systematically. The hydroxyl groups in the surface of CNF generate hydrogen bonds with the pen...

SummaryDrugs of abuse, like alcohol, modulate gene expression in reward circuits and consequently alter behavior. However, the in vivo cellular mechanisms through which alcohol induces lasting transcriptional changes are unclear. We show that Drosophila Notch/Su(H) signaling and the secreted fib...

SiO2-supported silyl chromate catalyst (UCC S-2 catalyst) is an important catalyst for the commercial production of polyethylene. Cann first reported a possible green synthesis route for the preparation of S-2 catalyst through transformation from Phillips catalyst by addition of triphenylsilanol...

The dwindling supply of fossil resources makes it interesting to find renewable resources for our everyday chemicals. 5-Hydroxymethylfurfural (HMF) is easily produced from fructose, although its isolation is not easy in view of its poor stability. More stable equivalents are its ethers or esters...

The influence of different parameters on the conversion of carbohydrates and biomass into the potential biofuel intermediate 5-bromomethylfurfural (BMF) has been studied. Our optimized conditions avoid the use of lithium salt additives, making this method cheaper and environmentally more benign ...

A series of 1-methyl-N-[(substituted-phenylmethylidene)-1H-benzimidazol-2-amines (4a–4g) were prepared via the formation of 1-methyl-1H-benzimidazol-2-amine (3), which was prepared by the cycloaddition of o-phenylenediamine (1) with cyanogen bromide in the presence of aqueous base followed by N...

Lewis acid (ZnI2) – promoted Mannich reaction of azetidin-2-one – tethered aldimine 3 with silylenol ether 4 in toluene at –20 °C afforded a diastereomeric mixture of β-amino acid esters 5 and 6 in ratio 65:35. Diastereomers 5 and 6 were chromatographically separated and their crystal struc...

Melanin concentrating hormone (MCH) receptor antagonists have been proposed as potential treatments of obesity. MCH receptor antagonists with a biphenylamine subunit have been reported previously at Schering-Plough. Herein, we report the discovery of bicyclo[4.1.0]heptanes as replacements for th...

In this study, the removal of bisphenol A (BPA) and phosphate in zero-valent iron activated persulfate (ZVI/PS) oxidation process was investigated. Activation of PS by ZVI mainly produces strong oxidizing sulfate radicals (SO4−) which can efficiently degrade organic contaminants. ZVI is ultimate...

Among calcium phosphate biomaterials, calcium phosphate bone cements (CPCs) have attracted increased attention because of their ability of self-setting in vivo and injectability, opening the new opportunities for minimally invasive surgical procedures. However, any surgical procedure carries pot...