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Staff Research

Yasmin Saad

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

Author : Yasmin Saad

Source : European Journal of Medicinal Chemistry 74 2014

Date of Publication : 01/2014

Abstract : 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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With the growing emphasis on collaborative and interdisciplinary science, Research Centers have become indispensable to highly ranked universities. They gain their importance from the outstanding role they play in enhancing the academic activities, in general, and post graduate reputation and scientific ranking in particular. Realizing this fact, Future University in Egypt (FUE) have decided and allocated sufficient funds and infrastructure to establish FUE Research Center (FUERC) having the following vision, mission, and goals
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FUE has maintained a highly reputable dental faculty over the years, therefore the development of the Dental Hospital is a step towards the FUE goal of providing the best dental academic programs
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