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Staff Researches

khairia M. Youssef

Design and synthesis of potential Ribonucleotide reductase enzyme (RNR) inhibitors as antileukemic and/or antiviral 2'-Deoxymethylene Nucleosides

Khairia Mohamed Ahmed Youssef

Prof. Dr. Eric J. Lien

Future Journal of Pharmaceutical Sciences

2015

In order to improve the antitumor and/or antiviral activities of existing nucleoside analogs, eight new compounds (9a,b, 14a,b, 15a,b and 16a,b) were designed and synthesized. Halogen atom were incorporated at the 2-position of the purine base to render the amino group at the 6-position less susceptible to metabolism by adenosine deaminase. A methylene group was introduced at the 2'-position following the lead of nucleoside antibiotics angustmycin A and neplanocin A. The two key intermediates 9a and 9b were prepared from guanosine after protection of the 3' and 5' hydroxyl groups and oxidation of the 2' hydroxyl group to the corresponding carbonyl group using swern method. The conversion of the carbonyl group to the methylene function was carried out by applying wittig reaction conditions. The final compounds 14 a,b, 15 a,b, 16 a,b were prepared by means of nonaqueous diazotization of 9a and 9b. The prepared compounds were subjected to in vitro antileukemic and antiviral activity upon a new L1210 cell line that is doubly resistant to both hydroxyurea and deoxyadenosine which was grown and characterized. The new compounds showed potent antileukemic activity.

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Curcumin Analogs with anticipated anticancer activityIten M. Fawzy1, Khairia M. Youssef¬¬1, Nasser S. M. Ismail2, J. Gullbo3 and Khaled A. M. Abouzid¬2.1Pharmaceutical chemistry Dept. Faculty of Pharmaceutical Sciences & Pharmaceutical Industries, Future University, Cairo, 12311, Egypt.

Khairia Mohamed Ahmed Youssef

FUE Journal

2015

Six novel curcumin analogs were designed, synthesized with 3,5-dibenzylidenepiperidin-4-one core moiety and three of them were evaluated for their antitumor activities in 5 different cell lines; [ovarian cancer (A2780), renal adenocarcinoma (ACHN), prostate cancer (PC-3), colorectal cancer (Hct-116) and a leukemic monocyte lymphoma (U937-GTB)]. Also in silico molecular docking was performed on the six curcumin analogs to predict their binding affinity to tubulin enzyme and their ability to destabilize microtubules through interaction energy docking scores compared to that of podophyllotoxin. Three of newly synthesized compounds were tested in vitro for their effect on tubulin polymerization.

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PAC, a novel curcumin analogue, has anti-breast cancer properties with higher efficiency on ER-negative cells

Khairia Mohamed Ahmed Youssef

Ensaf M. Al-Hujaily, Ameera Gaafar Mohamed, Ibtehaj Al-Sharif, Khairia M. Youssef and Pulicat S. Manogaran, et al.

Breast Cancer Res Treat (2010) 128:97–107

2010

We have investigated here the anti-breast cancer properties of two novel curcumin analogues, EAC and PAC. Apoptosis was assessed by the annexin V/propidium iodide (PI) assay on different breast cancer and normal cells. Immunoblotting analysis determined the effects of these agents on different apoptotic and oncogenic proteins. Furthermore, flow cytometry and Elispot were utilised to investigate the effects on the cell cycle and the production of cytokines, respectively. Breast cancer tumour xenografts were developed in nude mice. Finally, 18F-radiolabeled PAC and curcumin were produced to study their bioavailability and tissue biodistribution in mice. PAC is five times more efficient than curcumin and EAC in inducing apoptosis, mainly via the internal mitochondrial route. This effect was 10-fold higher against ER-negative as compared to ER-positive cells, and ectopic expression of ERa rendered ER-negative breast cancer cells more resistant to PAC.

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Synthesis of curcumin and ethylcurcumin bioconjugatesas potential antitumor agents,

Khairia Mohamed Ahmed Youssef

Reem I. Al-Wabli, Omaima M. AboulWafa, Khairia M. Youssef.

Med Chem Res (2012) 21: 874-890.

2011

Some new curcumin and ethylcurcumin bioconjugates with various functionalities supported on the curcumin skeleton were synthesized and evaluated for antitumor activity. Most of the newly synthesized compounds are more active than curcumin and ethyl curcumin but are less cytotoxic than the reference compound doxorubicin. Surprisingly, many of these compounds are not cytotoxic to noncancer cells. Compounds 5c, 5e, 5g, 5j, 6b, and 6g having 5-methylthiadiazole, 6-methoxy-benzothiazole, diethylaminoethyl and the usual alkylating bis(2- chloroethyl)amino moieties showed the highest cytotoxic activity against SK-MEL cancer cells. Compounds 5k, 6c, and 6g are less cytotoxic to KB cancer cells. Moreover, compounds 5c, 5e, 5j, 5k, 6d, 6e, 6f, and 6g showed cytotoxicity against BT-549 cancer cells with 5j being the most active compound. Curcumin and the new intermediate di-O-chloroacetylcurcumin (3a) were also cytotoxic against the same cell line but are less active than the target compounds. Compound 6b is the only one exhibiting cytotoxicity against SK-OV-3 cancer cells.

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Design and Synthesis of Novel Imatinib Analogs as Anti-Tumor Multi-Targeting Kinases.

Khairia Mohamed Ahmed Youssef

Iten M. Fawzy1, Khairia M. Youssef 1, Nasser S. M. Ismail2 , Deena S. Lasheen2 and Khaled A. M. Abouzid2

FUE International Conference of Pharmaceutical Sciences, February 9-11, 2015

2015

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Design and Synthesis of Novel Imatinib Analogs as Anti-Tumor Multi-Targeting Kinases.

Khairia Mohamed Ahmed Youssef

Iten M. Fawzy1, Khairia M. Youssef 1, Nasser S. M. Ismail2 , Deena S. Lasheen2 and Khaled A. M. Abouzid2

FUE International Conference of Pharmaceutical Sciences, February 9-11, 2015

2015

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Design and Synthesis and Biological evaluation of Novel Curcumin Analogs with anticipated anticancer activity

Khairia Mohamed Ahmed Youssef

Iten M. Fawzy1, Khairia M. Youssef¬¬1, Nasser S. M. Ismail2, J. Gullbo3 and Khaled A. M. Abouzid¬2.

Journal of Future of Pharmaceutical Sciences

2015

Extensive research conducted within past years revealed that curcumin is a highly pleiotropic molecule that interacts with a diverse range of molecular targets and hence it possess anti-proliferative activities against tumor cells.The great similarities between curcumin analogs and chalcones inspired their testing against tubulin enzyme activity as recent research revealed that chalcones possess cytotoxic activity associated with tubulin inhibition and interference with microtubule formation, which is essential in mitosis and cell replication.

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Design and synthesis of potential Ribonucleotide reductase enzyme (RNR) inhibitors as antileukemic and/or antiviral 2'-Deoxymethylene Nucleosides

Khairia Mohamed Ahmed Youssef

Eric J. Lien

Future Journal of Pharmaceutical Sciences

2015

In order to improve the antitumor and/or antiviral activities of existing nucleoside analogs, eight new compounds (9a,b, 14a,b, 15a,b and 16a,b) were designed and synthesized. Halogen atom were incorporated at the 2-position of the purine base to render the amino group at the 6-position less susceptible to metabolism by adenosine deaminase. A methylene group was introduced at the 2'-position following the lead of nucleoside antibiotics angustmycin A and neplanocin A. The two key intermediates 9a and 9b were prepared from guanosine after protection of the 3' and 5' hydroxyl groups and oxidation of the 2' hydroxyl group to the corresponding carbonyl group using swern method. The conversion of the carbonyl group to the methylene function was carried out by applying wittig reaction conditions. The final compounds 14a,b, 15a,b, 16a,b were prepared by means of nonaqueous diazotization of 9a and 9b. The prepared compounds were subjected to in vitro antileukemic and antiviral activity upon a new L1210 cell line that is doubly resistant to both hydroxyurea and deoxyadenosine which was grown and characterized. The new compounds showed potent antileukemic activity.

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Targeted Drug Delivery System (TDDS): Encapsulating Newly Synthesized Anti-cancer Compounds-Conjugated Gold Nanoparticles

Khairia Mohamed Ahmed Youssef

Khairia M. Youssef¬¬1, Nasser S. M.

OMICS International Pharma Middle East Conference

2015

Targeted drug delivery system(TDDS) is the most important research field for the design and development of pharmaceutical drugs. The basic premise of a TDDS is to concentrate the drug in the tissues of interest while reducing the relative concentration of medication in other remaining tissues [1, 2]. As a result, the drug is localized to a greater degree on the targeted site while leaving surrounding tissues unaffected. The ideal drug delivery system delivers drug at rates finely tuned to the biological requirement of the body sign and development [3, 4]. The significant advantage with TDDS includes protecting the payload and improving therapeutic index [4-6]. TDDS has several advantages for the treatment of disease quantitatively. For instance, drug localization, decreased side effects, reduced dosage, modulated pharmacokinetics, controlled bio-distribution, and most importantly, improved patient's compliance [7, 8]. In this context, TDDS, especially gold-based nanoparticles (AuNPs) will be used as a model system in this work. The main objective and basic principle behind the concept of targeting is that, the specific drug receptor is targeted to fit and improve their binding affinity, to the specific receptor that ultimately will trigger the pharmacological activity [9].

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Chemopreventive Effects of Curcumin Analogs in DMH-Induced Colon Cancer in Albino Rats Model.

Khairia Mohamed Ahmed Youssef

FUE Journal

2015

Synthesis and preclinical safety evaluation in mice and rats of Curcumin (1) and curcumin analogs (2, 3) were done. Besides, the chemopreventive effects in DMH-induced colon cancer in albino rats model were performed. Sections of mammary gland, heart, kidney, liver, spleen, and colon were done. Administration of the prophylactic treatment for four weeks before the induction of cancer by DMH, showed that compound 3 is the most active one. Chemopreventive treatment with different forms of curcumin extracts for 2 and 4 weeks caused a reduction in the number of aberrant crypt foci (ACF) especially compound 3. Chemopreventive treatment with different forms of curcumin extracts for 2 and 4 weeks caused a reduction in the number of tumor cells.

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Ribonucleotide reductase enzyme (RNR) inhibitors as antileukemic and/or antiviral 2'-Deoxymethylene Nucleosides. 1Dept. of Pharm. Chemistry, Faculty of Pharmaceutical Sciences and Pharmaceutical Industries, Future University, Cairo, Egypt. 12311.

Khairia Mohamed Ahmed Youssef

Future Journal of Pharmaceutical Sciences(FJPS), Cairo, Egypt (2014) In Press.

2014

In order to improve the antitumor and/or antiviral activities of existing nucleoside analogs, eight new compounds (9a,b, 14a,b, 15a,b and 16a,b) were designed and synthesized. Halogen atom were incorporated at the 2-position of the purine base to render the amino group at the 6-position less susceptible to metabolism by adenosine deaminase. A methylene group was introduced at the 2'-position following the lead of nucleoside antibiotics angustmycin A and neplanocin A. The two key intermediates 9a and 9b were prepared from guanosine after protection of the 3' and 5' hydroxyl groups and oxidation of the 2' hydroxyl group to the corresponding carbonyl group using swern method. The conversion of the carbonyl group to the methylene function was carried out by applying wittig reaction conditions. The final compounds 14 a,b, 15 a,b, 16 a,b were prepared by means of nonaqueous diazotization of 9a and 9b. The prepared compounds were subjected to in vitro antileukemic and antiviral activity upon a new L1210 cell line that is doubly resistant to both hydroxyurea and deoxyadenosine which was grown and characterized. The new compounds showed potent antileukemic activity.

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Simultaneous determination of ciprofloxacin hydrochloride and metronidazole in spiked human plasma by ultra performance liquid chromatography tandem mass spectroscopy. Asmaa Mandour1, 1Ramzeia Ismail1, Khairia M. Youssef1, Ehab El-Kady2. 1Dept. of Pharm. Chemistry, Faculty of Pharmaceutical Sciences and Pharmaceutical Industries, Future University, Cairo, Egypt.y

Khairia Mohamed Ahmed Youssef

FIP International Conference 2014 at Bangkok

2014

Simultaneous determination of ciprofloxacin hydrochloride and metronidazole in spiked human plasma by ultra performance liquid chromatography tandem mass spectroscopAsmaa

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