A series of 3-bromopyruvate (3-BP) derivatives were synthesized to develop new potent anticancer agents. The chemical structures the compounds characterized using FT-IR, 1 H-, 13 C-NMR spectroscopy, and elemental analysis (CHN). Their cytotoxic activities investigated against four cancer cell lines, including colon (SW1116), breast (MDA-MB-231), lung (A549), liver (HepG2) lines. Among compounds, 3b showed promising activity compared 3-BP, with IC50 values 16.3 μM, 19.1 27.8 14.5 μM A549,...

In a straightforward and fast protocol, mixture of 1,3-dimethylimidazolium fluoride ([DMIM]F) 1-butylimidazolium tetrafluoroborate ([Hbim]BF₄) efficiently catalyzed the reaction epoxides with ketene silyl acetals (KSA) to give various γ-lactones under metal-free conditions. Diverse kinds desired were directly prepared high regioselectivities yields in simple one-pot procedure using [DMIM]F as Si-O bond activator [Hbim]BF₄ solvent acidic ionic liquid catalyst. The was recovered reused three...

Marine sponge/oxalic acid was found to be an efficient catalyst for the imino Diels–Alder reaction of synthesized N-aryl-substituted aldimines and various alkenes provide 1,2-dihyro 1,2,3,4-tetrahydro-quinolines using 1,7-sigmatropic rearrangement with induction chirality. Mild conditions, simple experimental procedure, good yields products, optical active render this new method attractive reaction.

Background: Antacids are the most commonly used medications for fast symptomatic relief of gastric disorders. Because adverse effects, low efficiency and high cost some chemical antacids, identifying a natural medicine with seems useful. Therefore, aim present study was to prepare antacid tablets from Cuttlefish bone assessment its properties. Methods: 24 different formulations cuttlefish were prepared by direct compression using fillers (starch, cellulose, lactose, mixture those) in ratios...

AIDS, as a lethal disease, is caused by infection with the HIV virus that affects millions of people. Three essential enzymes should be encoded for replication virus: protease, integrase and reverse transcriptase (RT). RT has two different activities including DNA polymerase ribonuclease H (RNase H). However, all marketed inhibitors target only activity. Therefore, activity may serve new drug discovery. In present study, series 3-Hydroxypyrimidine-2, 4-dione derivatives potent RT-associated...

Marine sponge/nano-CuO as a natural catalyst efficiently catalyzed the Sulfonylation reaction of p-chlorobenzene sulfonyl chlorides with amines in order to prepare sulfonamides. The advantages included use catalyst, ease handling, requirement very small amount mild condition and appropriateness high yield.The current study aimed look for solid support develop general, novel method synthesize sulfonamides absence strong base, it was found that marine is efficient this at room temperature.The...

The synthesis of 3,6-bis(triphenylphosphonium) cyclohexene dichromate is described. This reagent oxidizes primary and secondary alcohols to their corresponding carbonyl compounds thiols disulfides, amines azo compounds.

Abstract One of the most effective approaches to discovering novel drugs for cancer treatment involves exploration new synthetic compounds. The pyrazinoic acid or pyrazine‐2‐carboxylic (PA)‐derivative compounds can be explored as a anticancer agent due their nitrogenous heteroaromatic ring. In this study, ten novels PA derivatives were synthesized by Ugi multicomponent reaction and characterized using IR, NMR, mass spectroscopy. cytotoxic activity was assayed in three different cell lines,...

Background: Alzheimer's disease (AD), the most typical type of dementia and memory loss, is a complicated progressive neurodegenerative disorder. Due to multi-factorial etiology AD, multi-target-directed ligand (MTDL) approach can be potential method in seeking new drug candidates for this disease. Methods: In study, over 200 tacrine-naphtoquinone hybrids have been designed their drug-likeness, molecular docking, descriptor analysis were conducted find out candidate with less toxicity better...

In this work, twenty different physical and chemical methods were used to study the effect of pretreatment on Cr(VI) Cd(II) biosorption by an aquatic plant (Ceratophyllum demersum) biomass.The H3PO4 boiled biomass had highest capacity (45 mg/g) for Cr(VI).The NaOH showed a higher (63 mg/g).Dunnett's test was carried out compare raw with those pretreated NaOH, results better performance samples.To explore surface characteristics explain differences in behavior; SEM, FT-IR elemental analysis...

A new and efficient method have been developed for the synthesis of different indole derivatives from various ketones, having at least one hydrogen atom attached to each their α-carbon atoms, hydrazines in solvent-free conditions, using marine sponge/H3PO4 as a naturally occurring chiral catalyst.This study recommended use catalyst preparation phenylhydrazones ketones α-hydrogen subsequent cyclisation products indoles.The reaction was carried out by mixing phenylhydrazine, ketone, powder...

: Background: Marine sponge/nano-CuO as a natural catalyst efficiently catalyzed the Sulfonylation reaction of p-chlorobenzene sulfonyl chlorides with amines in order to prepare sulfonamides. The advantages included use catalyst, ease handling, requirement very small amount mild condition and appropriateness high yield. Objectives: current study aimed look for solid support develop general, novel method synthesize sulfonamides absence strong base, it was found that marine is efficient this...

The expression of heat shock protein 27 (Hsp27) as a chaperone protein, is increased in response to various stress stimuli such anticancer chemotherapy. This phenomenon can lead survive the cells and causes drug resistance. In this study, series methanesulfonamide derivatives dual Hsp27 tubulin inhibitors treatment cancer were applied quantitative structure–activity relationship (QSAR) analysis. A collection chemometrics methods MLR, FA-MLR, PCR, GA-PLS was make relations between structural...

This study aimed to develop an oral succinyl chitosan-coated liposomal formulation containing grape seed extract and assess its therapeutic efficacy in rats with bleomycin-induced pulmonary fibrosis.N-succinyl chitosan was synthesized, the formulations were prepared characterized regarding phenolic content assay morphology. Size, zeta potential, vitro drug release, stability. Pulmonary fibrosis induced by intratracheal bleomycin injection, hydroxyproline measurements, lung weight, animal...

DNA double strand-breaks (DSBs) are the most deleterious lesions that can affect genome of living beings and lethal if not quickly properly repaired. Recently, N-phenyl ureidobenzenesulfonates (PUB-SOs) as tubulin inhibitors blocking cells cycle progression in S-phase inducing DSBs is discovered. Here, a set PUB-SOs derivatives were applied to quantitative structural activity relationship (QSAR) analysis. A series chemometrics methods like MLR, FA- PCR partial least squared included variable...

A new and efficient method have been developed for the synthesis of α,β-unsaturated carbonyl compounds from various aldehydes ketones, using marine calcinated coral/NaNO3 cuttlebone/NaNO3, as natural catalysts cross aldol condensation. The aim present study was to solids/NaNO3: catalyst Aldol materials were purchased Merck Aldrich Companies. IR spectra recorded on a Perkin-Elmer RXI infrared spectrometer. H NMR 400 MHz Brucker FT-NMR SEM image 1455 VP LEO-Germany. TLC accomplished purity...