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SYNTHESIS OF THIOGLYCOSIDES OF EXPECTED NOVEL BIOLOGICAL ACTIVITY
khairia M. Youssef
Professor of Pharmaceutical Organic Chemistry
Abstract
SYNTHESIS OF THIOGLYCOSIDES OF EXPECTED NOVEL BIOLOGICAL ACTIVITY
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ResearchesAwardsPublicationsWebSite DataPrevious PositionCertifications Please Fill In All Info In English Name * Place * Content Research Magazines Date * Invalid Date Documnet
English Name Publish Place Date Content Delete Edit Curcumin Analogs with anticipated anticancer activity FUE Journal 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. Design and synthesis of potential Ribonucleotide reductase enzyme (RNR) inhibitors as antileukemic and/or antiviral 2'-Deoxymethylene Nucleosides FUE Journal 2014 In order to improve the antitumor and/or antiviral activities of existing
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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. Chemopreventive Effects of Curcumin Analogs in DMH-Induced Colon Cancer in Albino Rats Model. FUE Journal 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. QSAR of Novel Hydroxyphenylureas as Antioxidant Agents QSAR& Combinatorial Sciences 2008 A set of descriptors consisting of quantum, chemical, and topological descriptors has been used for modeling the activity of novel hydroxyphenylureas to scavenge Free Radicals (FRs) produced by Peripheral Multinuclear Neutrophil Cells (PMNs) expressed as the rate of change per unit added volume of FR (Kapp min 1). Simple as well as multiple regressions have indicated that PW2 (Path\Walk-2-Randic Shape Index) is the most dominating parameter to be used in modeling Kapp. Excellent results are obtained in multiparametric regressions. The results are critically discussed using a variety of statistical parameters. The models are validated using Leave-One-Out (LOO) and Leave- Group-Out (LGO) crossvalidation, external test set, and chance correlation. 1 Introduction Active oxygen species and Free Radicals (FRs) have been recognized to play an important role in the initiation and/ or progression of various diseases such as ischemia-reperfusion injury, atherosclerosis, and inflammatory injury [1]. Antioxidants are expected to be promising drugs for the treatment of these diseases by removing oxidative stresses.
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The antioxidant chemopreventive activities of o-methoxyphenols of the curcumin [1,7-bis(4-hydroxy-3-methoxyphenyl)- 1,6-heptadien-3,5-dione] attract remarkable current interest because of its importance in biological systems [2±6]. Recent work by our laboratory identified that modification of groups on the terminal aromatic rings of curcumin reveals that electron-donating groups increase antioxidant activity [7, 8]. It was reported that uric acid scavenges radical species and the resultant urate radical is stabilized by delocalization of the unpaired electron in the p electron system containing urea substructures [9]. In addition, there are number of examples in which substituted phenols display Molecular docking and in silico ADME study of Novel N9-substituted Purines targeting CK1 and abl-tyrosine kinase Bangkok 2014 Novel N9-substitiuted purines were designed with anticipated anticancer activity based on the idea presented by recent publications were new compounds were synthesized combining the purine system in their structure in order to explore possible interactions with the different regions of the ATP binding site in several disease-related protein kinases especially cancer [1]. The study was supported by an in silico molecular docking study against both casein kinase-1 (CK1) and Bcr-abl-tyrosine kinase together with an in silico ADME study to assure the bioavailability of these compounds. 1 2 3
Please Fill In All Info In English Award Name * Award Date * wrong Reason * Award Place *
Award Name Award Date Reason Award Place Delete Edit AZAZI FUE Award for Outstanding Research 2013 Each year, FUE will recognize one full time professor for outstanding research and scholarship. The winner will be announced at the graduation ceremonies. An individual may nominate himself/herself or be nominated by another person. The emphasis of the award is on research achievement at FUE. Evaluation criteria will include research merit and its impact on the field; attainment of national and international recognition for superior scholarship through peer-reviewed publications; continued creativity over a sustained period; professional activities including editorial activity and academic awards; and the professional status of individuals providing supporting letters. Future University in Egypt 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
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analogs. 2010 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 the silver award from King Abdul Aziz city for science and technology for the exclusive research 2008 the silver award from King Abdul Aziz city for science and technology for the exclusive research ³Novel 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. King Abdul Aziz city for science and technology, Saudi Arabia 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. 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. Who's who in Science and Engineering, USA the Bronze award from King Abdul Aziz city for science and technology for the exclusive research ³Synthesis 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. 2010 For the exclusive research ³Synthesis 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
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SYNTHESIS OF THIOGLYCOSIDES OF EXPECTED NOVEL BIOLOGICAL ACTIVITY
- 2012, January
Abstract
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