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khairia M. Youssef

Basic information

Name : khairia M. Youssef
Title: Professor of Pharmaceutical Organic Chemistry
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Personal Info: Professor Khairia Youssef, Professor of Organic Chemistry, Department od Pharmaceutical Chemistry. • Dr. Khairia had the Bachelor of Pharmaceutical Sciences, the Master degree and Ph.D. in Organic Chemistry from Faculty of Pharmacy, Cairo University on 1977, 1980 and 1984, respectively. • On 1988, Dr. Khairia was on a special research assignment with Etreby Computer in Los Angeles, California, U.S.A. • On 1992, Dr. Khairia was on a Peace Fellowship for Post Doctoral Research which concerns with "Design and Synthesis of Potential Antileukemic and/or Antiviral 2'-Deoxymethylene Nucleosides" at the University of Southern California, Los Angeles, California. U.S.A., under the supervision of Dr. Eric J. Lien, Ph. D. The design of the work is based on QSAR. • Prof. Dr. Youssef is interested in drug design, synthesis and evaluation of certain pharmacologically active compounds. Prof. Youssef had been awarded the Bronze award from King Abdul Aziz city for science and technology for the exclusive research “Synthesis of Curcumin Analogues as Potential Antioxidant, Cancer Chemopreventive Agents” which had been granted by King Abdul Aziz city for science and technology, Project No. AR 19-39. Prof. Youssef had been awarded a certificate from The Marquis Who's who Publications Board as a subject of biographical record in Who's who in Science and Engineering 2008-2009. Inclusion in which is limited to those individuals who have demonstrated outstanding achievement in their own fields of endeavor and who have, thereby, contributed significantly to the betterment of contemporary society. She had been awarded the silver award from King Abdul Aziz city for science and technology for the exclusive research “Novel Modified Estrogens: Synthesis, Binding Affinity to Estrogen Receptor, Biological and Antitumor Activities of various Novel Modified Estrogen” which had been granted by King Abdul Aziz city for science and technology, Project No. AR 24-4. Prof. Youssef had been awarded the FUE Azazi Award for Outstanding Research for the academic year 2012/2013. This reflects well on the important contributions to the scholarly reputation of FUE. Perzigian, Anthony (perzigaj) [email protected] Prof. Youssef as an International Conference Organizer had been awarded a Certificate for Participating as Organizer for the 1st FUE International Conference on Pharmaceutical Technologies (1st FUE-ICPT), Feb, 2012.http://icpt.fue.edu.eg/ Also, Prof. Youssef had been awarded a Certificate for Participating as Organizer for 3rd FUE International Conference of Pharmaceutical Sciences (3rd FUE-ICPS), Feb, 9-11, 2015. http://www.fue.edu.eg/pharmaconference. Finally, Prof. Youssef was informed that the organizing committee of OMICS International Pharma Middle East Conference November 02-04, 2014, Dubai, UAE are pleased to join them and give a keynote presentation on: Targeted Drug Delivery System (TDDS): Encapsulating Newly Synthesized Anti-cancer Compounds-Conjugated Gold Nanoparticles Also, she was informed that the selection committee has decided to be one of the Conference Organizing Committee. www.conferenceseries.com View More...

Education

Certificate Major University Year
PhD Organic Chemistry Faculty of Pharmacy - Cairo University 1984
Masters Organic Chemistry Cairo University - Faculty of Pharmacy 1980
Bachelor . Cairo University - Faculty of Pharmacy 1977

Teaching Experience

Name of Organization Position From Date To Date
Faculty of Pharmaceutical Sciences and Pharmaceutical Industries, Future University in Egypt Professor of Pharmaceutical Organic Chemistry 01/01/2007 01/01/2016
Faculty of Pharmaceutical Sciences and Pharmaceutical Industries, Future University in Egypt Professor of Pharmaceutical Organic Chemistry 01/01/2007 01/01/2015
Faculty of Pharmacy, King Saud University, K.S.A. Professor at the Pharmaceutical Chemistry Department 01/01/2005 01/01/2007
College of Pharmacy, Science and Medical studies Department, King Saud University, K.S.A. Head of Pharmaceutical Chemistry Department 01/01/2002 01/01/2005
Faculty of Pharmacy, King Saud University Professor at Pharmaceutical Chemistry Department 01/01/1999 01/01/2002
Pharmaceutical Chemistry Department, Faculty of Pharmacy, King Saud University Associate Professor 01/01/1994 01/01/1999
Faculty of Pharmacy, Cairo University Assistant Professor at the Organic Chemistry Department 01/01/1992 01/01/1994
Faculty of Pharmacy, Cairo University Assistant Professor at the Organic Chemistry Department 01/01/1989 01/01/1991

Researches /Publications

Design, synthesis and molecular modeling study of certain VEGFR-2 inhibitors based on thienopyrimidine scaffold as cancer targeting agents - 01/0

Khairia Mohamed Ahmed Youssef

Khaled A.M. Abouzid

01/03/2019

Different series of novel thieno [2,3-d]pyrimidine derivative (9a-d,10a-f,l,m and 15a-m) were designed, synthesized and evaluated for their ability to in vitro inhibit VEGFR-2 enzyme. Also, the cytotoxicity of the final compounds was tested against a panel of 60 different human cancer cell lines by NCI. The VEGFR-2 enzyme inhibitory results revealed that compounds 10d, 15d and 15 g are among the most active inhibitors with IC50 values of 2.5, 5.48 and 2.27 µM respectively, while compound 10a remarkably showed the highest cell growth inhibition with mean growth inhibition (GI) percent of 31.57%. It exhibited broad spectrum anti-proliferative activity against several NCI cell lines specifically on human breast cancer (T7-47D) and renal cancer (A498) cell lines of 85.5% and 77.65% inhibition respectively. To investigate the mechanistic aspects underlying the activity, further biological studies like flow cytometry cell cycle together with caspase-3 colorimetric assays were carried on compound 10a. Flow cytometric analysis on both MCV-7 and PC-3 cancer cells revealed that it induced cell-cycle arrest in the G0-G1phase and reinforced apoptosis via activation of caspase-3. Furthermore, molecular modeling studies have been carried out to gain further understanding of the binding mode in the active site of VEGFR-2 enzyme and predict pharmacokinetic properties of all the synthesized inhibitors.

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Design, synthesis and molecular modeling study of certain VEGFR-2 inhibitors based on thienopyrimidne scaffold as cancer targeting agents. - 01/1

Khairia Mohamed Ahmed Youssef

Amna Ghith, Khairia M. Youssef , Nasser S. M. Ismail, Khaled A. M. Abouzid

01/11/2018

Different seriesof novel thieno [2,3-d]pyrimidine derivative (9a-d,10a-f,l,m and15a-m) were designed, synthesized and evaluated for their ability to in vitro inhibit VEGFR-2 enzyme. Also, the cytotoxicity of the final compounds was tested against a panel of 60 different human cancer cell lines by NCI. The VEGFR-2 enzyme inhibitoryresultsrevealedthatcompounds10d,15dand15gareamongthemostactiveinhibitorswithIC50 valuesof2.5,5.48and2.27µMrespectively,whilecompound10aremarkablyshowedthehighestcellgrowth inhibitionwithmeangrowthinhibition(GI)percentof31.57%.Itexhibitedbroadspectrumanti-proliferative activityagainstseveralNCIcelllinesspecificallyonhumanbreastcancer(T7-47D)andrenalcancer(A498)cell lines of 85.5% and 77.65% inhibition respectively. To investigate the mechanistic aspects underlying the activity,furtherbiologicalstudieslikeflowcytometrycellcycletogetherwithcaspase-3colorimetricassayswere carried on compound 10a. Flow cytometric analysis on both MCV-7 and PC-3 cancer cells revealed that it inducedcell-cyclearrestintheG0-G1phaseandreinforcedapoptosisviaactivationofcaspase-3.Furthermore, molecular modeling studies have been carried out to gain further understanding of the binding mode in the activesiteofVEGFR-2enzymeandpredictpharmacokineticpropertiesofallthesynthesizedinhibitors.

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N-substituted-piperidines as novel anti-alzheimer agents: Synthesis, antioxidant activity, and molecular docking study - 01/0

Khairia Mohamed Ahmed Youssef

01/06/2018

Design, synthesis and evaluation of new acetylcholinesterase inhibitors by combining carbamoylpiperidine analogs containing nipecotic acid scaffold were described. Then, a series of hybrids have been developed by introducing Free radical scavengers. Molecular modeling was performed and structure activity relationships are discussed. Among the series, most potent compounds showed effective AchE inhibitions, high selectivity over butyrylcholinesterase and high radical scavenging activities. On the basis of this work, the ability of analogs containing nipecotic acid scaffold to serve in the design of N-benzyl-piperidine linked multipotent molecules for the treatment of Alzheimer Disease.

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Design, synthesis and 3D QSAR based pharmacophore study of novel imatinib analogs as antitumor-apoptotic agents - 01/0

Khairia Mohamed Ahmed Youssef

Deena S Lasheen, Khaled AM Abouzid

01/05/2018

Aim: Imatinib possesses various mechanisms for combating cancer, making the development of imatinib analogs an attractive target for cancer research. Method: Two series of analogs were designed and synthesized, maintaining the essential pharmacophoric features in imatinib structure. The synthesized compounds were subjected to cell-based antiproliferative assays against nonsmall lung (A549) and colon cancer cell lines. In addition, flow cytometry cell cycle and caspase-3 colorimetric assays were performed. Results: Most compounds showed potent anticancer activity against both cell lines with IC50 = 0.14–5.07 μM. Three compounds demonstrated ability to reinforce cell cycle arrest at G1 stage in a manner similar to imatinib. In addition, they induced apoptosis via activation of caspase-3.

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67. Design, synthesis and 3D QSAR based pharmacophore study of novel imatinib analogs as antitumor-apoptotic agents. - 01/0

Khairia Mohamed Ahmed Youssef

Iten M Fawzy1, Khairia M Youssef1, Deena S Lasheen2, Nasser SM Ismail1 & Khaled AM Abouzid2

01/05/2018

Imatinib possesses various mechanisms for combating cancer, making the development of imatinib analogs an attractive target for cancer research. Method: Two series of analogs were designed and synthesized, maintaining the essential pharmacophoric features in imatinib structure. The synthesized compounds were subjected to cell-based antiproliferative assays against nonsmall lung (A549) and colon cancer cell lines. In addition, flow cytometry cell cycle and caspase-3 colorimetric assays were performed. Results: Most compounds showed potent anticancer activity against both cell lines with IC50 = 0.14–5.07 μM. Three compounds demonstrated ability to reinforce cell cycle arrest at G1 stage in a manner similar to imatinib. In addition, they induced apoptosis via activation of caspase-3.

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N-substituted-piperidines as Novel Anti-alzheimer Agents: Synthesis, - 01/1

Khairia Mohamed Ahmed Youssef

Iten M. Fawzy a, Hussein I. El-Subbagh

01/12/2017

Design, synthesis and evaluation of new acetylcholinesterase inhibitors by combining carbamoylpiperidine analogs containing nipecotic acid scaffold were described. Then, a series of hybrids have been developed by introducing Free radical scavengers. Molecular modeling was performed and structure activity relationships are discussed. Among the series, most potent compounds showed effective AchE inhibitions, high selectivity over butyrylcholinesterase and high radical scavenging activities. On the basis of this work, the ability of analogs containing nipecotic acid scaffold to serve in the design of Nbenzyl- piperidine linked multipotent molecules for the treatment of Alzheimer Disease.

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Medicinal Attributes of Thienopyrimidine Based Scaffold Targeting - 01/1

Khairia Mohamed Ahmed Youssef

Amna Ghith1, Nasser S.M. Ismail 1, Khaled A.M. Abouzid2

01/11/2017

Thienopyrimidines (TP), comprising a thiophene ring fused with pyrimidine, are famous bioisosteres to purines, an essential part of the human metabolome. This scaffold has become an interesting structural element in the development of pharmaceutical compounds, due to their wide spectrum applications as cytotoxic agents against different types of human cancer cell lines, cGMP phosphodiesterase inhibitors, and anti-viral, anti-inflammatory, and anti-microbial agents. The structural similarity of this scaffold with adenine made it an excellent moiety to be used in the design of kinase inhibitors. This review focuses on the chemistry of thienopyrimidine derivatives, their potential activities against various kinases, and their structure–activity relationship studies.

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Medicinal attributes of thienopyrimidine based scaffold targeting tyrosine kinases and their potential anticancer activities. - 01/0

Khairia Mohamed Ahmed Youssef

Khaled A.M. Abouzid

01/07/2017

Thienopyrimidines (TP), comprising a thiophene ring fused with pyrimidine, are famous bioisosteres to purines, an essential part of the human metabolome. This scaffold has become an interesting structural element in the development of pharmaceutical compounds, due to their wide spectrum applications as cytotoxic agents against different types of human cancer cell lines, cGMP phosphodiesterase inhibitors, and anti‐viral, anti‐inflammatory, and anti‐microbial agents. The structural similarity of this scaffold with adenine made it an excellent moiety to be used in the design of kinase inhibitors. This review focuses on the chemistry of thienopyrimidine derivatives, their potential activities against various kinases, and their structure–activity relationship studies.

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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. - 01/1

Khairia Mohamed Ahmed Youssef

01/12/2015

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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Design and synthesis of potential Ribonucleotide reductase enzyme (RNR) inhibitors as antileukemic and/or antiviral 2'-Deoxymethylene Nucleosides - 01/1

Khairia Mohamed Ahmed Youssef

Prof. Dr. Eric J. Lien

01/12/2015

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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Design and Synthesis and Biological evaluation of Novel Curcumin Analogs with anticipated anticancer activity - 01/0

Khairia Mohamed Ahmed Youssef

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

01/01/2015

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 - 01/0

Khairia Mohamed Ahmed Youssef

Eric J. Lien

01/01/2015

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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Chemopreventive Effects of Curcumin Analogs in DMH-Induced Colon Cancer in Albino Rats Model. - 01/0

Khairia Mohamed Ahmed Youssef

01/01/2015

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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Chemopreventive Effects of Curcumin Analogs in DMH-Induced Colon Cancer in Albino Rats Model. - 01/0

Khairia Mohamed Ahmed Youssef

01/01/2014

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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Design and Synthesis and Biological evaluation of Novel Curcumin Analogs with anticipated anticancer activity - 01/0

Khairia Mohamed Ahmed Youssef

01/01/2014

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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Design and synthesis and biological evaluation of novel curcumin analogs with anticipated anticancer activity.Iten M. Fawzy1, Khairia M. Youssef¬¬1, Nasser S. M. Ismail2, J. Gullbo3 and Khaled A. M. Abouzid. Al- Azhar University Magazine for Pharmaceutical Publications- July 2013. - 01/0

Khairia Mohamed Ahmed Youssef

01/01/2013

Analogs Ia-g, IIa-d, IIIa-d and IVa-e represent four different series of compounds designed and synthesized with 3,5-dibenzylidenepiperidin-4-one core moiety. Results: Compounds showed interaction energy comparable to or within the range of podophyllotoxin itself when docked into the colchicine binding site of tubulin using the podophyllotoxin-tubulin complex (PDB 1SA1).

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Molecular Modeling of Novel Curcumin Analogs with Anticipated Anticancer Activity.Iten M. Fawzy, Khairia M. Youssef, Nasser S. M. Ismail, Khaled A. M. Abouzid. 1Pharmaceutical chemistry Dept. Faculty of Pharmaceutical Sciences & Pharmaceutical Industries, Future University, Cairo, 12311, Egypt. - 01/0

Khairia Mohamed Ahmed Youssef

01/01/2012

Molecular Modeling of Novel Curcumin Analogs with Anticipated Anticancer Activity Iten M. Fawzy, Khairia M. Youssef, Nasser S. M. Ismail, Khaled A. M. Abouzid

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Synthesis of curcumin and ethylcurcumin bioconjugatesas potential antitumor agents, - 01/0

Khairia Mohamed Ahmed Youssef

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

01/02/2011

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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Synthesis, antiplatelet aggregation activity, and molecularmodeling study of novel substituted-piperazine analogues. Khairia M. Youssef • Mohamed A. Al-Omar • Hussein I. El-Subbagh • Laila A. Abou-zeid • Abdel-Galil M. Abdel-Gader • - 01/0

Khairia Mohamed Ahmed Youssef

01/01/2011

New carbamoylpyridine and carbamoylpiperidine analogues containing nipecotic acid scaffold were designed, synthesized, and evaluated for their platelet aggregation inhibitory activity. Molecular modeling investigation was performed and the impact of lipophilicity on activity was also discussed. Structure activity relationship among this series was obtained. N1-[1-(4-bromobenzyl)-3-piperidinocarbonyl]- N4-(2-chlorophenyl)-piperazine hydrobromide (20), and 1,4-bis-[3-[N4-(2-chlorophenyl)-N1-(piperazinocarbonyl)]- piperidin-1-yl-methyl]-benzene dibromide (30) are the most active antiplatelet aggregating compounds in this study, both at concentration of 0.06 lM.

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PAC, a novel curcumin analogue, has anti-breast cancer properties with higher efficiency on ER-negative cells - 01/0

Khairia Mohamed Ahmed Youssef

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

01/08/2010

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, antiplatelet aggregation activity, and molecular - 01/0

Khairia Mohamed Ahmed Youssef

01/01/2010

New carbamoylpyridine and carbamoylpiperidine analogues containing nipecotic acid scaffold were designed, synthesized, and evaluated for their platelet aggregation inhibitory activity. Molecular modeling investigation was performed and the impact of lipophilicity on activity was also discussed. Structure activity relationship among this series was obtained. N1-[1-(4-bromobenzyl)-3-piperidinocarbonyl]- N4-(2-chlorophenyl)-piperazine hydrobromide (20), and 1,4-bis-[3-[N4-(2-chlorophenyl)-N1-(piperazinocarbonyl)]- piperidin-1-yl-methyl]-benzene dibromide (30) are the most active antiplatelet aggregating compounds in this study, both at concentration of 0.06 lM.

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Awards

Award Donor Date
AZAZI FUE Award for Outstanding Research Future University in Egypt 2013
the Bronze award from King Abdul Aziz city for science and technology for the exclusive research “Synthesis of Curcumin Analogues as Potential Antioxidant, Cancer Chemopreventive Agents” which had been granted by King Abdul Aziz city for science and technology, Project No. AR 19-39. King Abdul Aziz city for science and technology 2010
D. Walid Bin Amin El-Kayaly For Scintific Research award- Saudy Pharmaceutical Syndicate, for the research titled: Synthesis, dihydrofolate reductase inhibition, antitumor testing, and molecular modeling study of some new 4(3H)-quinazolinone analogs. El-Kayaly For Scintific Research award- Saudy Pharmaceutical Syndicate, Saudi Arabia 2010
A certificate from The Marquis Who's who Publications Board as a subject of biographical record in Who's who in Science and Engineering 2008-2009. Who's who in Science and Engineering, USA 2009
the silver award from King Abdul Aziz city for science and technology for the exclusive research King Abdul Aziz city for science and technology, Saudi Arabia 2008

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