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Staff Researches

Hanan Refaat

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Hanan Mohamed Refaat Khalil Elaassy

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Global Dean's Forum

2015

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Solid-Phase Synthesis and Anti-Tumor Evaluation of Novel Benzimidazole Derivatives

Hanan Mohamed Refaat Khalil Elaassy

Hanan M. Refaat* 1, Mohamed Mohsen Ismail 2, Mona Mounir Kamel 3, Mohamed Tawfeek Mohamed 3

75th FIP World Congress of Pharmacy and Pharmaceutical Sciences

2015

The benzimidazole skeleton, when selectively functionalized, is considered building block for the preparation of potent antineoplastic agents. 2- Substituted benzimidazole-5-carboxylic acids and 4- or 5- carboxylic acid derivatives that were used in the design of antineoplastic agents[1]. On the other hand, solid phase organic chemistry offers the opportunity of synthesizing molecules via novel routes, which may be difficult or impossible using traditional solution method[2][3]. In this work, we report an improved synthesis of selected novel 1,2- disubstituted benzimidazole-5-carboxylic acid analogues via solid phase to examine the feasibility of polymer-support method in synthesis of biologically active benzimidazoles. All of the synthesized compounds were docked on the active site of deoxyribonucleic acid to test their binding affinities. Furthermore, the synthesized compounds were subjected to preliminary screening of their antineoplastic activity.

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Application of resin-bound reagents for the synthesis of benzimidazole derivatives

Hanan Mohamed Refaat Khalil Elaassy

Ismail, M. Mohsen; Kamel, Mona M.; Nemr, M. Tawfik Mohamed

Journal of Chemical Research

2016

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Synthesis and anti-inflammatory activity of some 3, 5-diaryl-2-pyrazoline derivatives

Hanan Mohamed Refaat Khalil Elaassy

Omneya M. Khalil and Hanan M. Refaat

Oriental Journal of Chemistry

2011

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Hanan Mohamed Refaat Khalil Elaassy

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3rd International Conference on Pharmaceutical Sciences

2015

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Novel thiazolopyrane and thiazolopyranopyrimidine derivatives carrying a sulfonamide moiety of expected cytotoxic and radiosensitizing Activities

Hanan Mohamed Refaat Khalil Elaassy

Mostafa M. Ghorab, Mohamed A. Shaaban, Hanan M. Refaat, Helmy I. Heiba, Sara S. Ibrahim

Journal of Materials Science and Engineering

2011

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Synthesis, anticancer activity and effects on cell cycle profile and apoptosis of novel thieno[2,3-d]pyrimidine and thieno[3,2-e] triazolo[4,3-c]pyrimidine derivatives.

Hanan Mohamed Refaat Khalil Elaassy

M. M. Kandeel, Hanan M. Refaat, Asmaa E. Kassab, Inas G.Shahin and Tamer M. Abdelghany

European Journal of Medicinal Chemistry,

2015

Motivated by the widely reported anticancer activity of thieno[2,3-d]pyrimidines a series of 24 new 2-substitutedhexahydrocycloocta[4,5] thieno[2,3-d]pyrimidines with different substituents at C-4 position and hexahydrocycloocta[4,5]thieno[3,2-e]-1,2,4-triazolo[4,3-c]pyrimidines were synthesized. The anticancer activity of 17 compounds were evaluated by National Cancer Institute (USA) using a two stage process utilizing 59 different human tumor cell lines representing leukemia, melanoma, cancers of lung, colon, central nervous system (CNS), ovary, kidney, prostate as well as breast. Compound 9c showed broad spectrum potent anticancer activity in nano molar to micro molar range against 56 human tumor cell lines with GI50 less than 10 μM ranging from 0.495 to 5.57 μM, also it is worth mentioning that compound 9c had the marked highest selectivity against the two cell lines T-47D and MDA-MB-468 belonging to breast cancer with GI50 = 0.495 and 0.568 μM respectively, and its effect was further studied on cell cycle progression and induction of apoptosis in the MDA-MB-468 cell line. Results showed that compound 9c induced cell cycle arrest at G2/M phase and also, showed accumulation of cells in pre-G1 phase which may result from, degradation or fragmentation of the genetic materials indicating a possible role of apoptosis in compound 9c-induced cancer cell death and cytotoxicity and verifying this compound as promising selective anticancer lead. Compound 6c was selective against K-562, SR and MOLT-4 cell lines belonging to leukemia showing growth inhibition percentages 86.38, 65.76 and 60.40 at a single dose test, at the same time it showed lethal activity against HOP-92 representing non-small cell lung cancer. Interestingly, leukemia SR, CNS cancer SNB-75 and renal cancer UO-31 cell lines proved to be sensitive to compound 6d with growth inhibition percentages 52.86, 50.94 and 53.99 respectively. Additionally, compound 6d demonstrated lethal activity to HOP-92 belonging non-small cell lung cancer.

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FUE International Conference on Pharmaceutical Sciences

Hanan Mohamed Refaat Khalil Elaassy

Cairo

2013

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3rd International Scientific Conference of Faculty of Pharmacy Cairo University

Hanan Mohamed Refaat Khalil Elaassy

Cairo

2012

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FUE International Conference on Pharmaceutical Sciences

Hanan Mohamed Refaat Khalil Elaassy

Cairo

2012

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Synthesis of potential anticancer derivatives of pyrido[1,2-a] benzimidazoles

Hanan Mohamed Refaat Khalil Elaassy

Medicinal Chemistry Research

2012

18. Synthesis of potential anticancer derivatives of pyrido[1,2-a] benzimidazoles; Hanan M. Refaat; Medicinal Chemistry Research, 21(7), 1253–1260 (2012)

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Anticancer and radiosensitizing evaluation of some new pyranothiazole-Schiff bases bearing the biologically active sulfonamide moiety

Hanan Mohamed Refaat Khalil Elaassy

European Journal of Medicinal Chemistry

2012

19. Anticancer and radiosensitizing evaluation of some new pyranothiazole-Schiff bases bearing the biologically active sulfonamide moiety; Mostafa M. Ghorab, Mohamed A. Shaaban, Hanan M. Refaat, Helmy I. Heiba, Sara S. Ibrahim; European Journal of Medicinal Chemistry, 53 (7), 403-407 (2012).

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