E. S. Nossier

Biological Validation of Novel Polysubstituted Pyrazole Candidates with in Vitro Anticancer Activities

With the aim of developing novel antitumor scaffolds, a novel series of polysubstituted pyrazole derivatives linked to different nitrogenous heterocyclic ring systems at the C-4 position were synthesized through different chemical reactions and characterized by means of spectral and elemental analyses and their antiproliferative activity against 60 different human tumor cell lines was validated by the U.S. National Cancer Institute using a two stage process. The in vitro anticancer evaluation revealed that compound 9 showed increased potency toward most human tumor cell lines with GI50MG-MID = 3.59 µM, as compared to the standard drug sorafenib (GI50 MG-MID = 1.90 µM). At the same time, compounds 6a and 7 were selective against the HOP-92 cell line of non-small cell lung cancer with GI50 1.65 and 1.61 µM, respectively.

Design and Synthesis of Novel Pyrazole-Substituted Different Nitrogenous Heterocyclic Ring Systems as Potential Anti-Inflammatory Agents

With the aim of developing novel anti-inflammatory scaffolds, a new series of pyrazole-substituted various nitrogenous heterocyclic ring systems at C-4 position were synthesized through different chemical reactions and validated by means of spectral and elemental data. The new obtained compounds were investigated for their anti-inflammatory activity using the carrageenan-induced paw edema standard technique and revealed that, compound 6b showed increased potency with % inhibition of edema 85.23 ± 1.92 and 85.78 ± 0.99, respectively, higher than the standard reference drugs indomethacin and celebrex (72.99% and 83.76%). Molecular modeling studies were initiated herein to validate the attained pharmacological data and provide understandable evidence for the observed anti-inflammatory behavior.

Synthesis, reactions, and antimicrobial activity of some novel fused thiazolo[3,2-a]pyrimidine-5H-indeno[1,2-d]pyrimidine derivatives

Series of novel substituted thioxopyrimidine and thiazolo[3,2-a]pyrimidine compounds that combine various heteroaryl rings have been synthesized via Biginelli one-pot three-component reaction and elucidated with chemical and spectral analysis. Several products were tested for their antimicrobial properties.

Synthesis of some novel S-alkylated and S-glycosylated hydantoin derivatives containing pyrene moiety

Abstract3-Aryl-5-[(Z)-pyrenylmethylene]-2-alkylthiohydantoins and 3-Aryl-5-[(Z)-pyrenylmethylene]-2-(D-glycosyl)-2-thiohydantoins functionalized with different aromatic and glycoside substituents have been synthesized by the reaction of (Z)-3-(4-methoxyphenyl)-5-[(pyren-8-yl)methylene]-2-thiohydantoin with alkyl halides, cyclic and acyclic nucleosides via various routes with moderate to good yields and characterized by 1H, 13C NMR and mass spectra and elemental analysis

Synthesis and characterization of novel 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) and dihydro-alkylthio-benzyloxopyrimidine (S-DABO) analogs containing a benzo[d]thiazol moiety

A series of novel dihydro-alkylthio-benzyloxopyrimidine (S-DABO) and 1-[(2-hydroxyethoxy) methyl]-6-(phenylthio)thymine (HEPT) analogs bearing a (benzo[d]thiazol-2-yl)methyl moiety at the C6 position of the pyrimidine core have been synthesized. 5-Allyl-6-{(benzo[d]thiazol-2-yl)methyl}-2-thiouracil and 5-allyl-6-{(benzo-[d]thiazol-2-yl)methyl}uracil were alkylated to give, respectively, S2- and N1- ethoxymethyl and -methylthiomethyl uracil derivatives. 5-Allyl-6-[(benzo[d]thiazol-2-yl)methyl]-2-thiouracil was also alkylated by S2 with methyl bromoacetate and hydrolyzed to the corresponding acid.

Synthesis, characterization, and antimicrobial activity of some chiral linear carboxamides with incorporated peptide linkage

A new group of chiral linear 7-methyl-4-oxo-1,8-naphthyridine-3-carboxamides with incorporated peptide linkage have been synthesized via condensation of 1-ethyl-N-(1-hydrazinyl-3-methyl-1-oxobutan-2-yl)-7-methyl–4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxamide with various derivatives of sugar pentose, acetophenones and thiosemicarbazide. Structures of the products were elucidated by spectroscopic methods and chemical analysis. Antimicrobial properties of the synthesized compounds were tested.

Synthesis and some reactions of novel (4Z)-4-{[1-(3-chlorophenyl)-3-(4-methoxyphenyl)-1H-pyrazol-4-yl]methylene}-2-hydrazinyl-1-phenyl-1H-imidazol-5(4H)-ones

Some novel (4Z)-2-[(E)-2-arylidenehydrazinyl]-4-{[1-(3-chlorophenyl)-3-(4-methoxyphenyl)-1H-pyrazol-4-yl]methylene}-1-phenyl-1H-imidazol-5(4H)-ones have been synthesized in a one-pot threecomponent cyclocondensation of pyrazole-4-carbaldehyde derivative with glycine and different isothiocyanate derivatives. The structures of the newly synthesized compounds were characterized by analytical and spectral data.

Synthesis and characterization of new pyrazolyl-substituted thiazolidinone, thiazole, and thiazoline candidates

Abstract1-(3-Chlorophenyl)-3-(4-methoxyphenyl)-1H-pyrazole-4-carbaldehyde was used in preparation of (E)-1-{[1-(3-chlorophenyl)-3-(4-methoxyphenyl)-1H-pyrazol-4-yl]methylene}thiosemicarbazide. Its following reaction with ethyl bromoacetate, diethyl 2-bromomalonate, phenacyl bromide, and maleic anhydride gave pyrazolyl pharmacophore linked thiazole, thiazoline and thiazolidinone-5-carboxylic acid derivatives.

Synthesis of some new pyrazolyl-thiazolidinone derivatives starting from 1-(3-chlorophenyl)-3-(4-methoxyphenyl)-1H-pyrazole-4-carboxaldehyde

A novel synthetic approach to (E)-1-{[1-(3-chlorophenyl)-3-[(4-methoxyphenyl-1H-pyrazol-4-yl)- methylene]hydrazono}-3-phenylthiazolidin-4-one starting from the key intermediate thiosemicarbazone derivative is presented. The latter compound reacted with some aromatic and heterocyclic aldehydes to give (1-{[1-(3-chlorophenyl)-3-(4-methoxyphenyl)-1H-pyrazol-4-yl]methylene}hydrazono)-5-(substituted benzylidene)-3-phenylthiazolidin-4-one derivatives.

Efficient Synthesis and Reactions of New Functionally Substituted Pyrido[2,3-d]pyrimidine Candidates

Pyrido[2,3-d]pyrimidine derivatives were synthesized by the reaction of 2-hydrazinopyrido[2,3-d]-pyrimidin-4(3H)-one with different aryl aldehydes and active methylene compounds. Their structures were characterized by spectroscopic methods.