Abstract (Benzimidazol-2-yl)-7-hydroxycoumarin and N -(2-hydroxyphenyl)-7-hydroxycoumarin-3-carbo... more Abstract (Benzimidazol-2-yl)-7-hydroxycoumarin and N -(2-hydroxyphenyl)-7-hydroxycoumarin-3-carboxamide have been synthesized by the condensation of ethyl 7-hydroxycoumarin-3-carboxylate in acetic acid. Acetylation with acetic anhydride and halogenation with bromine in acetic acid’s presence of the previous compounds has yielded the corresponding acetoxy and dibromo derivatives. The synthesized molecules that contain coumarin ring have been evaluated for their activities against breast cancer and they have shown good in vitro antiproliferative activities against a human breast cancer line (MCF-7). The results have shown that 3-(benzimidazol-2-yl)-7-acetoxycoumarin had a significant cytotoxic effect compared to the standard DOX (doxorubicin) drug.
A novel series of 3,4-disubstitutued coumarin derivatives have been synthesized by the reaction o... more A novel series of 3,4-disubstitutued coumarin derivatives have been synthesized by the reaction of ethyl coumarin-3-carboxylate with pyrazole-3,5-dione and condensation of ethyl 7-hydroxycoumarin-3-carboxylate with 4,6-dibromo-3-amino phenol. Acylation with acetic anhydride and condensation of coumarin derivatives with 2-hydroxybenzaldehyde yielded the corresponding acetyl derivatives and 4-substituted pyrazole derivatives. Structures of the synthesized compounds were elucidated by spectral methods and elemental analysis. All the prepared derivatives were evaluated for their cytotoxicity against human breast carcinoma cell line (MCF-7). Compound VI showed the least IC 50 value in MTT colorimetric assay as compared to that of the standard marketed drug staurosporin.
Background: Early cardiovascular disease (CVD) management and prediction have become mandatory in... more Background: Early cardiovascular disease (CVD) management and prediction have become mandatory in children with chronic kidney disease (CKD). Association between neutrophil gelatinase-associated lipocalin (NGAL) and CVD events in pediatric CKD patients remains unclear. Thus, we aimed to evaluate this relationship and to clarify the association between NGAL serum levels and some CVD related parameters. Subjects and methods: A total of 70 children patients with CKD (30 with and 40 without CVD). The patient’s data were retrospectively recorded from the medical files of each patient. NGAL serum levels were measured by ELISA commercial kits. Association between different parameters was assessed by the Pearson correlation coefficient. Results: NGAL serum levels were significantly (P<0.0001) higher in patients with CVD (2450 (1335-2880) pg/mL) than patients without CVD (371 (285-1363) pg/mL) and healthy controls (295 (166-357) pg/mL). At 1300 pg/mL, NGAL has a good CVD predictive functi...
ABSTRACT 7- or 9-substituted-2-amino-4-hydroxy-7-methoxy-5H-chromeno-[4,3-d]-pyrimidine-5-one, 3a... more ABSTRACT 7- or 9-substituted-2-amino-4-hydroxy-7-methoxy-5H-chromeno-[4,3-d]-pyrimidine-5-one, 3a,b, were prepared via cyclocondensation of 6- or 8-substituted-3-ethoxycarbonyl coumarin, 2, with guanidine hydrochloride in presence of anhydrous potassium carbonate. Acetylation and alkylation of compounds with acetic anhydride and ω-bromomethyl aryl ketones yielded the corresponding N-acetyl derivatives, 4a,b, and 8- or 10-substituted-5-hydroxy-1-p-tolyl-6-H-chromeno[3,4-e] imidazo[1,2-a] pyrimidine-6-one, 5a,b,. Treatment of compound 3a with ethylchloroacetate and methyl acrylate afforded the corresponding benzopyrano-[4,3-d]-imidazolidino-[2,1-b]-pyrimidine, 6, and benzopyrano-[4,3-d]-pyrimidino-[2,1-b]-pyrimidine, 7, respectively. Some of the new compounds were evaluated for cytotoxicity activity against a hepatocellular carcinoma cell line.
Abstract (Benzimidazol-2-yl)-7-hydroxycoumarin and N -(2-hydroxyphenyl)-7-hydroxycoumarin-3-carbo... more Abstract (Benzimidazol-2-yl)-7-hydroxycoumarin and N -(2-hydroxyphenyl)-7-hydroxycoumarin-3-carboxamide have been synthesized by the condensation of ethyl 7-hydroxycoumarin-3-carboxylate in acetic acid. Acetylation with acetic anhydride and halogenation with bromine in acetic acid’s presence of the previous compounds has yielded the corresponding acetoxy and dibromo derivatives. The synthesized molecules that contain coumarin ring have been evaluated for their activities against breast cancer and they have shown good in vitro antiproliferative activities against a human breast cancer line (MCF-7). The results have shown that 3-(benzimidazol-2-yl)-7-acetoxycoumarin had a significant cytotoxic effect compared to the standard DOX (doxorubicin) drug.
A novel series of 3,4-disubstitutued coumarin derivatives have been synthesized by the reaction o... more A novel series of 3,4-disubstitutued coumarin derivatives have been synthesized by the reaction of ethyl coumarin-3-carboxylate with pyrazole-3,5-dione and condensation of ethyl 7-hydroxycoumarin-3-carboxylate with 4,6-dibromo-3-amino phenol. Acylation with acetic anhydride and condensation of coumarin derivatives with 2-hydroxybenzaldehyde yielded the corresponding acetyl derivatives and 4-substituted pyrazole derivatives. Structures of the synthesized compounds were elucidated by spectral methods and elemental analysis. All the prepared derivatives were evaluated for their cytotoxicity against human breast carcinoma cell line (MCF-7). Compound VI showed the least IC 50 value in MTT colorimetric assay as compared to that of the standard marketed drug staurosporin.
Background: Early cardiovascular disease (CVD) management and prediction have become mandatory in... more Background: Early cardiovascular disease (CVD) management and prediction have become mandatory in children with chronic kidney disease (CKD). Association between neutrophil gelatinase-associated lipocalin (NGAL) and CVD events in pediatric CKD patients remains unclear. Thus, we aimed to evaluate this relationship and to clarify the association between NGAL serum levels and some CVD related parameters. Subjects and methods: A total of 70 children patients with CKD (30 with and 40 without CVD). The patient’s data were retrospectively recorded from the medical files of each patient. NGAL serum levels were measured by ELISA commercial kits. Association between different parameters was assessed by the Pearson correlation coefficient. Results: NGAL serum levels were significantly (P<0.0001) higher in patients with CVD (2450 (1335-2880) pg/mL) than patients without CVD (371 (285-1363) pg/mL) and healthy controls (295 (166-357) pg/mL). At 1300 pg/mL, NGAL has a good CVD predictive functi...
ABSTRACT 7- or 9-substituted-2-amino-4-hydroxy-7-methoxy-5H-chromeno-[4,3-d]-pyrimidine-5-one, 3a... more ABSTRACT 7- or 9-substituted-2-amino-4-hydroxy-7-methoxy-5H-chromeno-[4,3-d]-pyrimidine-5-one, 3a,b, were prepared via cyclocondensation of 6- or 8-substituted-3-ethoxycarbonyl coumarin, 2, with guanidine hydrochloride in presence of anhydrous potassium carbonate. Acetylation and alkylation of compounds with acetic anhydride and ω-bromomethyl aryl ketones yielded the corresponding N-acetyl derivatives, 4a,b, and 8- or 10-substituted-5-hydroxy-1-p-tolyl-6-H-chromeno[3,4-e] imidazo[1,2-a] pyrimidine-6-one, 5a,b,. Treatment of compound 3a with ethylchloroacetate and methyl acrylate afforded the corresponding benzopyrano-[4,3-d]-imidazolidino-[2,1-b]-pyrimidine, 6, and benzopyrano-[4,3-d]-pyrimidino-[2,1-b]-pyrimidine, 7, respectively. Some of the new compounds were evaluated for cytotoxicity activity against a hepatocellular carcinoma cell line.
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Papers by Amal Moustafa