Design, synthesis and antitumor evaluation of some purine based derivatives / (Record no. 80538)
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| 000 -LEADER | |
|---|---|
| fixed length control field | 03405cam a2200349 a 4500 |
| 003 - CONTROL NUMBER IDENTIFIER | |
| control field | EG-GiCUC |
| 005 - DATE AND TIME OF LATEST TRANSACTION | |
| control field | 20250223032724.0 |
| 008 - FIXED-LENGTH DATA ELEMENTS--GENERAL INFORMATION | |
| fixed length control field | 210405s2021 ua f m 000 0 eng d |
| 040 ## - CATALOGING SOURCE | |
| Original cataloging agency | EG-GiCUC |
| Language of cataloging | eng |
| Transcribing agency | EG-GiCUC |
| 041 0# - LANGUAGE CODE | |
| Language code of text/sound track or separate title | eng |
| 049 ## - LOCAL HOLDINGS (OCLC) | |
| Holding library | Deposite |
| 097 ## - Thesis Degree | |
| Thesis Level | Ph.D |
| 099 ## - LOCAL FREE-TEXT CALL NUMBER (OCLC) | |
| Classification number | Cai01.08.05.Ph.D.2021.Ab.D |
| 100 0# - MAIN ENTRY--PERSONAL NAME | |
| Personal name | Abdalla Reda Mohamed |
| 245 10 - TITLE STATEMENT | |
| Title | Design, synthesis and antitumor evaluation of some purine based derivatives / |
| Statement of responsibility, etc. | Abdalla Reda Mohamed ; Supervised Nagwa Mohamed Abdelgawad , Hanan Hanna Georgey , Riham Francois George |
| 246 15 - VARYING FORM OF TITLE | |
| Title proper/short title | تصميم و تشييد و تقييم الفاعلية المضادة للأورام لبعض المشتقات المعتمدة على البيورين |
| 260 ## - PUBLICATION, DISTRIBUTION, ETC. | |
| Place of publication, distribution, etc. | Cairo : |
| Name of publisher, distributor, etc. | Abdalla Reda Mohamed , |
| Date of publication, distribution, etc. | 2021 |
| 300 ## - PHYSICAL DESCRIPTION | |
| Extent | 173 P. ; |
| Dimensions | 25cm |
| 502 ## - DISSERTATION NOTE | |
| Dissertation note | Thesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry |
| 520 ## - SUMMARY, ETC. | |
| Summary, etc. | In light of the molecular reciprocity between the Ras/Raf//MEK/ERK and PI3K/Akt/mTOR pathways, which are considered as major players in tumorigenesis, and together provide cancer cells with the ability to withstand when targeting only one pathway of them. Aiming to tackle the growing antitumor resistance, and to maintain an efficient antiproliferative leverage, a compromised approach between ligand and structure based drug design was utilized to select thirty two compounds, 7,8-disubstituted-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione derivatives, for organic synthesis. The synthesized novel compounds satisfied certain criteria related to insights of modeling studies and crystal structures regards to several oncogenes such as of PI3K and B-Raf.Subsequently, all the synthesized compounds were evaluated for their in vitro anticancer activity according to the US-NCI protocol. Compounds 158 and 163c displayed potent and accepted benchmark according to DTP-NCI and further evaluated in the five doses assay. In addition to their pronounced and prominent antiproliferative activities, their cytotoxic effect against normal WI-38 cell line has been assessed, which revealed non-significant toxicity compared to sorafenib (34). Since the endeavor of the present study is to imbed antitumor efficacy through modulation of biological network, the rebound of multi-kinases targeting were also evaluated. Compounds with the highest mean growth inhibitions percent, were screened in vitro against PI3KÜ and B-RafV600E biological targets which showed potent activities. Compound 155 was found to be the most active in PI3KÜ inhibition with IC50 of 8.46 nM, while compound 157 showed superiority to inhibit the mutant type B-RafV600E with IC50 of 99.6 nM. Interestingly, compounds 158 and 163c anticancer effectiveness was consolidated by inhibition of B-RafWT, EGFR and VEGFR-2 with sub-micromolar IC50, in addition to their PI3KÜ and B-RafV600E inhibitory activities. Their predicted physicochemical and pharmacokinetic properties were also mentioned |
| 530 ## - ADDITIONAL PHYSICAL FORM AVAILABLE NOTE | |
| Additional physical form available note | Issued also as CD |
| 653 #4 - INDEX TERM--UNCONTROLLED | |
| Uncontrolled term | Anticancer |
| 653 #4 - INDEX TERM--UNCONTROLLED | |
| Uncontrolled term | Multi-kinase targeting |
| 653 #4 - INDEX TERM--UNCONTROLLED | |
| Uncontrolled term | Xanthine |
| 700 0# - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Hanan Hanna Georgey , |
| Relator term | |
| 700 0# - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Nagwa Mohamed Abdelgawad , |
| Relator term | |
| 700 0# - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Riham Francois George , |
| Relator term | |
| 856 ## - ELECTRONIC LOCATION AND ACCESS | |
| Uniform Resource Identifier | <a href="http://172.23.153.220/th.pdf">http://172.23.153.220/th.pdf</a> |
| 905 ## - LOCAL DATA ELEMENT E, LDE (RLIN) | |
| Cataloger | Nazla |
| Reviser | Revisor |
| 905 ## - LOCAL DATA ELEMENT E, LDE (RLIN) | |
| Cataloger | Shimaa |
| Reviser | Cataloger |
| 942 ## - ADDED ENTRY ELEMENTS (KOHA) | |
| Source of classification or shelving scheme | Dewey Decimal Classification |
| Koha item type | Thesis |
| Source of classification or shelving scheme | Not for loan | Home library | Current library | Date acquired | Full call number | Barcode | Date last seen | Koha item type | Copy number |
|---|---|---|---|---|---|---|---|---|---|
| Dewey Decimal Classification | المكتبة المركزبة الجديدة - جامعة القاهرة | قاعة الرسائل الجامعية - الدور الاول | 11.02.2024 | Cai01.08.05.Ph.D.2021.Ab.D | 01010110083190000 | 22.09.2023 | Thesis | ||
| Dewey Decimal Classification | المكتبة المركزبة الجديدة - جامعة القاهرة | مخـــزن الرســائل الجـــامعية - البدروم | 11.02.2024 | Cai01.08.05.Ph.D.2021.Ab.D | 01020110083190000 | 22.09.2023 | CD - Rom | 83190.CD |