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Staff Researches

Yasmin Saad

Non Classical Antifolates, Part 5. Benzodiazepine Analogs as a New Class of DHFR Inhibitors: Synthesis, Antitumor Testing and Molecular Modeling Study

Yasmin Saad Abulfadl Okasha

European Journal of Medicinal Chemistry 74 2014

2014

A new series of tetrahydro quinazoline and tetrahydro 1H dibenzo diazepine analogs were synthesized and tested for their DHFR inhibition and in vitro antitumor activity. Compound 35 showed a remarkable DHFR inhibitory potency which is twenty fold more active than methotrexate (MTX). Compounds 17 and 23 proved to be fifteen fold more active than the known antitumor 5 FU, with MG MID GI50, TGI and LC50 values of 1.5, 46.8, 93.3 and 1.4, 17.4, 93.3 respectively. Computer modeling studies allowed the identification that methoxy and methyl substituents, the system of the chalcone core, the nitrogen atoms, on the dibenzodiazepine ring as pharmacophoric features essential for activity. These mark points could be used as template model for further future optimization.

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Nonclassical antifolates, part 5. Benzodiazepine analogues as a new class of DHFR inhibitors: Synthesis, antitumor testing and molecular modeling study☆

Yasmin Saad Abulfadl Okasha

2013

A new series of tetrahydro-quinazoline and tetrahydro-1H-dibenzo[b,e][1,4]diazepine analogues were synthesized and tested for their DHFR inhibition and in- vitro antitumor activity. Compound 35 showed a remarkable DHFR inhibitory potency (IC50, 0.004 μM) which is twenty fold more active than methotrexate (MTX). Compounds 17 and 23 proved to be fifteen fold more active than the known antitumor 5-FU, with MG-MID GI50, TGI, and LC50 values of 1.5, 46.8, 93.3 and 1.4, 17.4, 93.3 μM, respectively. Computer modeling studies allowed the identification that methoxy and methyl substituents, the π-system of the chalcone core, the nitrogen atoms, on the dibenzodiazepine ring as pharmacophoric features essential for activity. These mark points could be used as template model for further future optimization.

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Nonclassical antifolates, Part 4. 5-(2-Aminothiazol-4-yl)-4-phenyl-4H-1,2,4-triazole-3-thiols as a new class of DHFR inhibitors: Synthesis, biological evaluation and molecular modeling study.

Yasmin Saad Abulfadl Okasha

2013

A new series of tetrahydro-quinazoline and tetrahydro-1H-dibenzo[b,e][1,4]diazepine analogues were synthesized and tested for their DHFR inhibition and in- vitro antitumor activity. Compound 35 showed a remarkable DHFR inhibitory potency (IC50, 0.004 μM) which is twenty fold more active than methotrexate (MTX). Compounds 17 and 23 proved to be fifteen fold more active than the known antitumor 5-FU, with MG-MID GI50, TGI, and LC50 values of 1.5, 46.8, 93.3 and 1.4, 17.4, 93.3 μM, respectively. Computer modeling studies allowed the identification that methoxy and methyl substituents, the π-system of the chalcone core, the nitrogen atoms, on the dibenzodiazepine ring as pharmacophoric features essential for activity. These mark points could be used as template model for further future optimization.

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ICPT

Yasmin Saad Abulfadl Okasha

FUE University

2012

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Effect of nigella sativa oil constituents on colon cancer

Yasmin Saad Abulfadl Okasha

2010

Effect of nigella sativa oil constituents on colon cancer egyptian society of toxicology

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Non

Yasmin Saad Abulfadl Okasha

2009

Non

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Effect of nigella sativa oil constituents on colon cancer

Yasmin Saad Abulfadl Okasha

helwan university

2009

effect of nigella sativa oil constituents on colon cancer

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