The 2-benzylidenecyclohexanone derivatives have been used as starting material to form a series o... more The 2-benzylidenecyclohexanone derivatives have been used as starting material to form a series of novel pyran, pyridine, pyrazole and thiophene derivatives. New approaches based on the reactivity of the starting materials towards different chemical reagents were developed and evaluated. Thirty one compounds of all the synthesized structures were selected and evaluated as significant anti-cancer agents. The results showed that some compounds with high activities towards the six cancer cell lines, NUGC (gastric cancer), DLDI (colon cancer), HA22T (liver cancer), HEPG2 (liver cancer), HONEI (nasopharyngeal carcinoma), HR (gastric cancer), MCF (breast cancer), WI38 (normal fibroblast cells) and comparing the results to inhibitory compound reference, CHS828.
Background: Due to their biological applications, many tetrahydrobenzo[d]thiazole derivatives wer... more Background: Due to their biological applications, many tetrahydrobenzo[d]thiazole derivatives were considered the most important class of heterocyclic compounds. There are many drugs known in the market containing the thiazole moiety responsible for the high drug activity. Objective: This work aimed to produce novel heterocyclic compounds such as pyrazole, isoxazole, thiophene, chromeno[7,8-d]thiazole, and thiazolo[4,5-h]quinoline derivatives. The newly synthesized heterocyclic compounds were evaluated against anticancer cell lines followed by c-Met enzymatic activity and tyrosine kinases inhibition for the most active compounds. Methods: In this work, the 3-phenyl-2-thioxo-2,3,5,6-tetrahydrobenzo[d]thiazol-7(4H)-one (3) was synthesized through the reaction of cyclohexane-1,3-dione with phenyl isothiocyanate and elemental sulfur. Compound 3 showed interesting activity toward some chemical reagents producing new heterocyclic compounds that can not be obtained another way. The newly s...
The chemical composition and biological activity of three parts (rind, flesh and seeds) of pumpki... more The chemical composition and biological activity of three parts (rind, flesh and seeds) of pumpkin fruits (Cucurbita pepo L.) cultivated in Egypt were studied. Chemical analysis of fibre, protein, β-carotene, carbohydrates, minerals and fatty acids present in the rind, flesh, seeds and defatted seeds meal was conducted. Chemical, GC-MS and biological assays of organic extracts of the main fruit parts, rind and flesh established their unique constituents. Chromatographic purification of the extracts afforded triglyceride fatty acid mixture (1), tetrahydro-thiophene (2), linoleic acid (3), calotropoleanly ester (4), cholesterol (5) and 13(18)-oleanen-3-ol (6). GC-MS analysis of the extract's unpolar fraction revealed the existence of dodecane and tetradecane. Structures of the isolated compounds (1–6) were confirmed by NMR and EI-MS spectrometry. Antimicrobial, antiviral and antitumour activities of the fruit parts were discussed. The promising combined extract of rind and flesh w...
The investigation of drugs used for the treatment of inflammatory diseases with limited side effe... more The investigation of drugs used for the treatment of inflammatory diseases with limited side effects becomes an urgent need for inflammation patients. This search aimed at the preparation of novel hybrid heterosteroids with structures especially non-ulcerogenic and anti-inflammatory activities. The heterocyclic steroids were formulated using simple and effective techniques. IR, H NMR, C NMR spectra and elemental microanalysis were used to characterize the synthesized compound. The in vivo anti-inflammatory activity of some of these compounds was studied using carrageenan-induced paw oedema assay. Also, the effect of the different compounds on the development of gastric mucosal damage induced in rats by 96% EtOH administration was studied. The most marked and sustained inhibition of the oedema response was observed with the administration of the low and high doses (25 and 50 mg/kg) of compounds 8, 4, 23, 14 as well as by the high dose of compound 32. There was no significant differen...
Many novel thiazole derivatives were designed and synthesized using 4-phenylthiazol-2-amine. The ... more Many novel thiazole derivatives were designed and synthesized using 4-phenylthiazol-2-amine. The reactivity of the latter compound toward different chemical reagents was studied. The structure of the newly synthesized compounds was established based on elemental analysis and spectral data. Furthermore, twenty compounds of the synthesized systems were selected and evaluated in (μM) as significant anticancer agents towards three human cancer cell lines [MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer), and SF-268 (CNS cancer)] and normal fibroblasts human cell line (WI-38). The results showed that compounds 9 and 14a displayed higher effeciency than the reference doxorubicin.
Purpose The purpose of this paper is to prepare new disperse dyes and apply for dying polyester f... more Purpose The purpose of this paper is to prepare new disperse dyes and apply for dying polyester fabrics. Design/methodology/approach The synthetic reaction was carried out through two steps: preparation of arylhydrazones and alkylation using enaminone and dimethylaminovinyl-pyridazine. The high temperature method was used to apply these dyes to polyester fibres. Findings The study revealed that there is a significant effect of the new prepared disperse dyes on polyester fabrics. The structures of the prepared dyes were established based on elemental analysis and spectral data (infra red (IR), mass spectrometry (MS) and proton nuclear magnetic resonance (1H-NMR), carbon 13th nuclear magnetic resonance (13C-NMR)). Research limitations/implications Disperse dyes containing heterocyclic moiety have attracted great academic and industrial attention owing to their significant. The potential of using disperse dyes easily prepared from arylhydrazones are promise broad applications for these...
Attempting to produce cyclized systems with potential anti-proliferative activity, a series of no... more Attempting to produce cyclized systems with potential anti-proliferative activity, a series of novel thiophene and benzothiophene derivatives were designed and synthesized. The reactivity of the latter derivatives towards different chemical reagents was studied. Twenty-one compounds were synthesized and evaluated as anti-cancer agents. The results showed that ethyl 5-amino-3-(4-chlorostyryl)-4-cyanothiophene-2-carboxylate (5b), ethyl 5-amino-4-((4-methoxyphenyl)carbonyl)-3-methylhiophene-2-carboxylate (8c) and 5-3-(ethoxy-3-oxopropanamido)-3-methyl-4-(phenylcarbamoyl)thiophene-2-carboxylate (9) were the most active compounds towards three tumor cell lines – MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer) and SF-268 (CNS cancer) and a normal fibro-blast human cell line (WI-38) compared to the anti-proliferative effects of the reference control doxorubicin.
Several novel pyrazolo[1,5‐a]pyrimidine derivatives containing two arylazo functions were synthes... more Several novel pyrazolo[1,5‐a]pyrimidine derivatives containing two arylazo functions were synthesised from 4‐arylazo‐3,5‐diaminopyrazoles. Such derivatives were used as starting components. The characteristics of and the application properties of the dyes synthesised from 4‐arylazo‐3,5‐diaminopyrazoles were investigated and reported.
The 2-benzylidenecyclohexanone derivatives have been used as starting material to form a series o... more The 2-benzylidenecyclohexanone derivatives have been used as starting material to form a series of novel pyran, pyridine, pyrazole and thiophene derivatives. New approaches based on the reactivity of the starting materials towards different chemical reagents were developed and evaluated. Thirty one compounds of all the synthesized structures were selected and evaluated as significant anti-cancer agents. The results showed that some compounds with high activities towards the six cancer cell lines, NUGC (gastric cancer), DLDI (colon cancer), HA22T (liver cancer), HEPG2 (liver cancer), HONEI (nasopharyngeal carcinoma), HR (gastric cancer), MCF (breast cancer), WI38 (normal fibroblast cells) and comparing the results to inhibitory compound reference, CHS828.
Background: Due to their biological applications, many tetrahydrobenzo[d]thiazole derivatives wer... more Background: Due to their biological applications, many tetrahydrobenzo[d]thiazole derivatives were considered the most important class of heterocyclic compounds. There are many drugs known in the market containing the thiazole moiety responsible for the high drug activity. Objective: This work aimed to produce novel heterocyclic compounds such as pyrazole, isoxazole, thiophene, chromeno[7,8-d]thiazole, and thiazolo[4,5-h]quinoline derivatives. The newly synthesized heterocyclic compounds were evaluated against anticancer cell lines followed by c-Met enzymatic activity and tyrosine kinases inhibition for the most active compounds. Methods: In this work, the 3-phenyl-2-thioxo-2,3,5,6-tetrahydrobenzo[d]thiazol-7(4H)-one (3) was synthesized through the reaction of cyclohexane-1,3-dione with phenyl isothiocyanate and elemental sulfur. Compound 3 showed interesting activity toward some chemical reagents producing new heterocyclic compounds that can not be obtained another way. The newly s...
The chemical composition and biological activity of three parts (rind, flesh and seeds) of pumpki... more The chemical composition and biological activity of three parts (rind, flesh and seeds) of pumpkin fruits (Cucurbita pepo L.) cultivated in Egypt were studied. Chemical analysis of fibre, protein, β-carotene, carbohydrates, minerals and fatty acids present in the rind, flesh, seeds and defatted seeds meal was conducted. Chemical, GC-MS and biological assays of organic extracts of the main fruit parts, rind and flesh established their unique constituents. Chromatographic purification of the extracts afforded triglyceride fatty acid mixture (1), tetrahydro-thiophene (2), linoleic acid (3), calotropoleanly ester (4), cholesterol (5) and 13(18)-oleanen-3-ol (6). GC-MS analysis of the extract's unpolar fraction revealed the existence of dodecane and tetradecane. Structures of the isolated compounds (1–6) were confirmed by NMR and EI-MS spectrometry. Antimicrobial, antiviral and antitumour activities of the fruit parts were discussed. The promising combined extract of rind and flesh w...
The investigation of drugs used for the treatment of inflammatory diseases with limited side effe... more The investigation of drugs used for the treatment of inflammatory diseases with limited side effects becomes an urgent need for inflammation patients. This search aimed at the preparation of novel hybrid heterosteroids with structures especially non-ulcerogenic and anti-inflammatory activities. The heterocyclic steroids were formulated using simple and effective techniques. IR, H NMR, C NMR spectra and elemental microanalysis were used to characterize the synthesized compound. The in vivo anti-inflammatory activity of some of these compounds was studied using carrageenan-induced paw oedema assay. Also, the effect of the different compounds on the development of gastric mucosal damage induced in rats by 96% EtOH administration was studied. The most marked and sustained inhibition of the oedema response was observed with the administration of the low and high doses (25 and 50 mg/kg) of compounds 8, 4, 23, 14 as well as by the high dose of compound 32. There was no significant differen...
Many novel thiazole derivatives were designed and synthesized using 4-phenylthiazol-2-amine. The ... more Many novel thiazole derivatives were designed and synthesized using 4-phenylthiazol-2-amine. The reactivity of the latter compound toward different chemical reagents was studied. The structure of the newly synthesized compounds was established based on elemental analysis and spectral data. Furthermore, twenty compounds of the synthesized systems were selected and evaluated in (μM) as significant anticancer agents towards three human cancer cell lines [MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer), and SF-268 (CNS cancer)] and normal fibroblasts human cell line (WI-38). The results showed that compounds 9 and 14a displayed higher effeciency than the reference doxorubicin.
Purpose The purpose of this paper is to prepare new disperse dyes and apply for dying polyester f... more Purpose The purpose of this paper is to prepare new disperse dyes and apply for dying polyester fabrics. Design/methodology/approach The synthetic reaction was carried out through two steps: preparation of arylhydrazones and alkylation using enaminone and dimethylaminovinyl-pyridazine. The high temperature method was used to apply these dyes to polyester fibres. Findings The study revealed that there is a significant effect of the new prepared disperse dyes on polyester fabrics. The structures of the prepared dyes were established based on elemental analysis and spectral data (infra red (IR), mass spectrometry (MS) and proton nuclear magnetic resonance (1H-NMR), carbon 13th nuclear magnetic resonance (13C-NMR)). Research limitations/implications Disperse dyes containing heterocyclic moiety have attracted great academic and industrial attention owing to their significant. The potential of using disperse dyes easily prepared from arylhydrazones are promise broad applications for these...
Attempting to produce cyclized systems with potential anti-proliferative activity, a series of no... more Attempting to produce cyclized systems with potential anti-proliferative activity, a series of novel thiophene and benzothiophene derivatives were designed and synthesized. The reactivity of the latter derivatives towards different chemical reagents was studied. Twenty-one compounds were synthesized and evaluated as anti-cancer agents. The results showed that ethyl 5-amino-3-(4-chlorostyryl)-4-cyanothiophene-2-carboxylate (5b), ethyl 5-amino-4-((4-methoxyphenyl)carbonyl)-3-methylhiophene-2-carboxylate (8c) and 5-3-(ethoxy-3-oxopropanamido)-3-methyl-4-(phenylcarbamoyl)thiophene-2-carboxylate (9) were the most active compounds towards three tumor cell lines – MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer) and SF-268 (CNS cancer) and a normal fibro-blast human cell line (WI-38) compared to the anti-proliferative effects of the reference control doxorubicin.
Several novel pyrazolo[1,5‐a]pyrimidine derivatives containing two arylazo functions were synthes... more Several novel pyrazolo[1,5‐a]pyrimidine derivatives containing two arylazo functions were synthesised from 4‐arylazo‐3,5‐diaminopyrazoles. Such derivatives were used as starting components. The characteristics of and the application properties of the dyes synthesised from 4‐arylazo‐3,5‐diaminopyrazoles were investigated and reported.
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