Background and methods: In a continuous combat against cancer which is one of the leading causes ... more Background and methods: In a continuous combat against cancer which is one of the leading causes of mortality now, chalcone and Schiff bases moieties have been incorporated and their antiproliferative activities and associated mechanisms against liver (HepG2) and breast (MCF-7) cell lines in addition to normal fibroblasts (WI-38) have been examined. Results: Derivatives 4 and 5 of Schiff bases only and chalcone derivatives of Schiff bases 1 and 2 were devoid of any antiproliferative activity. All three compounds (3, 6, and 7) with significant antiproliferative activity were selective and caused no growth inhibition in normal fibroblasts. Derivative 3 was a chalcone only with IC50 of ~20 μM and has a very interesting signature where it enhanced apoptosis in HepG2 by stimulating the expression of downstream execution caspase 3 without affecting neither p53 nor initiator caspase 9. In spite of the structural similarity between compounds 6 and 7, compound 6 discerned itself with a uniqu...
Three novel series of pyridine derivatives, namely Schiff's bases, 4-thiazolidinones and azet... more Three novel series of pyridine derivatives, namely Schiff's bases, 4-thiazolidinones and azetidin-2-ones bearing pyrazolo[3,4-b]pyridine moiety, have been synthesized. The chemical structures of the synthesized compounds were characterized. The compounds were tested for their antimicrobial activity using the agar well diffusion and broth macrodilution methods. The compounds were also evaluated for their antiproliferative activity using the sulforhodamine B (SRB) assay. The majority of the tested compounds exhibited slight to high antimicrobial activity against the test microorganisms with minimum inhibitory concentrations (MICs) of 0.12-62.5 µg/mL when compared to that of 3 standard antimicrobial agents (Ampicillin, 0.007-0.03 µg/mL; Gentamicin; 0.015-0.24 µg/mL; and Amphotericin B, 0.03-0.98 µg/mL). Compound (7b) was found to be nearly as active as the standard antimicrobial drug Amphotericin B against Fusarium oxysporum fungal strain with MIC of 0.98 µg/mL. Some of the test co...
Extending our work [1-11] on the reaction of organophosphorus reagents with different carbonyl fu... more Extending our work [1-11] on the reaction of organophosphorus reagents with different carbonyl functions. We examined the reactions of organophosphorus reagents towards substituted 3-cyano-2-pyridones which are important intermediates in the pharmaceutical, ...
2-Amino-7-hydroxy-4-(3,4-dimethoxyphenyl)-4H-chromene-3-carbonitrile has been synthesized and uti... more 2-Amino-7-hydroxy-4-(3,4-dimethoxyphenyl)-4H-chromene-3-carbonitrile has been synthesized and utilized to construct a variety of new heterocyclic systems such as chromenopyrimidines, chromeno-oxazinone, chromenotriazolopyrimidinethiones, oxopyrazole derivative, chromenotetrazolopyrimidine via reactions with phenyl isothiocyanate, hydrazine hydrate in ethanol at room and refluxing temperatures, formamide and carbon disulfide in ethanolic potassium hydroxide and pyridine respectively. Some of the synthesized compounds have been found potent as antifungal and antibacterial.
3,5-Dichloro-2-hydroxyacetophenone has been utilized as synthon for the synthesis of 4-methyl-3- ... more 3,5-Dichloro-2-hydroxyacetophenone has been utilized as synthon for the synthesis of 4-methyl-3- cyanocoumarin and chromone-3-carboxaldehyde derivatives. The reactivity of both coumarinic and chromonic heterocyclic systems towards different electrophiles and nucleophiles have been studied. Antibacterial and antifungal activity of selected coumarin and chromone derivatives has been screened. The biological study revealed that chromonic derivatives have more inhibitory action than coumarinic ones as well as some of the former namely; chromenopyrazole has inhibitory effect more than the standard Amphorericin B.
A facile one-pot four-component reaction was utilized to construct 2-oxo-1,2-dihydropyridine-3-ca... more A facile one-pot four-component reaction was utilized to construct 2-oxo-1,2-dihydropyridine-3-carbonitrile as a scaffold for the synthesis of many fused heterocyclic systems, namely, furopyridine, pyridothiadiazepinthione, and pyridotriazine, as well as non-fused heterocyclic systems such as phthalazin-2(1H)-ylnicotinonitrile, pyridin-2-yl-1H-pyrazole, and pyrazol-1-ylnicotino-nitrile,1-(3-cyanopyridin-2-yl)-1H-pyrazole. The new compounds were evaluated as antimicrobial and antiviral agents.
Background and methods: In a continuous combat against cancer which is one of the leading causes ... more Background and methods: In a continuous combat against cancer which is one of the leading causes of mortality now, chalcone and Schiff bases moieties have been incorporated and their antiproliferative activities and associated mechanisms against liver (HepG2) and breast (MCF-7) cell lines in addition to normal fibroblasts (WI-38) have been examined. Results: Derivatives 4 and 5 of Schiff bases only and chalcone derivatives of Schiff bases 1 and 2 were devoid of any antiproliferative activity. All three compounds (3, 6, and 7) with significant antiproliferative activity were selective and caused no growth inhibition in normal fibroblasts. Derivative 3 was a chalcone only with IC50 of ~20 μM and has a very interesting signature where it enhanced apoptosis in HepG2 by stimulating the expression of downstream execution caspase 3 without affecting neither p53 nor initiator caspase 9. In spite of the structural similarity between compounds 6 and 7, compound 6 discerned itself with a uniqu...
Three novel series of pyridine derivatives, namely Schiff's bases, 4-thiazolidinones and azet... more Three novel series of pyridine derivatives, namely Schiff's bases, 4-thiazolidinones and azetidin-2-ones bearing pyrazolo[3,4-b]pyridine moiety, have been synthesized. The chemical structures of the synthesized compounds were characterized. The compounds were tested for their antimicrobial activity using the agar well diffusion and broth macrodilution methods. The compounds were also evaluated for their antiproliferative activity using the sulforhodamine B (SRB) assay. The majority of the tested compounds exhibited slight to high antimicrobial activity against the test microorganisms with minimum inhibitory concentrations (MICs) of 0.12-62.5 µg/mL when compared to that of 3 standard antimicrobial agents (Ampicillin, 0.007-0.03 µg/mL; Gentamicin; 0.015-0.24 µg/mL; and Amphotericin B, 0.03-0.98 µg/mL). Compound (7b) was found to be nearly as active as the standard antimicrobial drug Amphotericin B against Fusarium oxysporum fungal strain with MIC of 0.98 µg/mL. Some of the test co...
Extending our work [1-11] on the reaction of organophosphorus reagents with different carbonyl fu... more Extending our work [1-11] on the reaction of organophosphorus reagents with different carbonyl functions. We examined the reactions of organophosphorus reagents towards substituted 3-cyano-2-pyridones which are important intermediates in the pharmaceutical, ...
2-Amino-7-hydroxy-4-(3,4-dimethoxyphenyl)-4H-chromene-3-carbonitrile has been synthesized and uti... more 2-Amino-7-hydroxy-4-(3,4-dimethoxyphenyl)-4H-chromene-3-carbonitrile has been synthesized and utilized to construct a variety of new heterocyclic systems such as chromenopyrimidines, chromeno-oxazinone, chromenotriazolopyrimidinethiones, oxopyrazole derivative, chromenotetrazolopyrimidine via reactions with phenyl isothiocyanate, hydrazine hydrate in ethanol at room and refluxing temperatures, formamide and carbon disulfide in ethanolic potassium hydroxide and pyridine respectively. Some of the synthesized compounds have been found potent as antifungal and antibacterial.
3,5-Dichloro-2-hydroxyacetophenone has been utilized as synthon for the synthesis of 4-methyl-3- ... more 3,5-Dichloro-2-hydroxyacetophenone has been utilized as synthon for the synthesis of 4-methyl-3- cyanocoumarin and chromone-3-carboxaldehyde derivatives. The reactivity of both coumarinic and chromonic heterocyclic systems towards different electrophiles and nucleophiles have been studied. Antibacterial and antifungal activity of selected coumarin and chromone derivatives has been screened. The biological study revealed that chromonic derivatives have more inhibitory action than coumarinic ones as well as some of the former namely; chromenopyrazole has inhibitory effect more than the standard Amphorericin B.
A facile one-pot four-component reaction was utilized to construct 2-oxo-1,2-dihydropyridine-3-ca... more A facile one-pot four-component reaction was utilized to construct 2-oxo-1,2-dihydropyridine-3-carbonitrile as a scaffold for the synthesis of many fused heterocyclic systems, namely, furopyridine, pyridothiadiazepinthione, and pyridotriazine, as well as non-fused heterocyclic systems such as phthalazin-2(1H)-ylnicotinonitrile, pyridin-2-yl-1H-pyrazole, and pyrazol-1-ylnicotino-nitrile,1-(3-cyanopyridin-2-yl)-1H-pyrazole. The new compounds were evaluated as antimicrobial and antiviral agents.
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Papers by Marwa Salem