Design and synthesis of some fused pyrimidine derivatives with potential activity against cancer kinome / (Record no. 83877)
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| 000 -LEADER | |
|---|---|
| fixed length control field | 03333cam a2200349 a 4500 |
| 003 - CONTROL NUMBER IDENTIFIER | |
| control field | EG-GiCUC |
| 005 - DATE AND TIME OF LATEST TRANSACTION | |
| control field | 20250223032910.0 |
| 008 - FIXED-LENGTH DATA ELEMENTS--GENERAL INFORMATION | |
| fixed length control field | 220108s2021 ua d 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.Me.D |
| 100 0# - MAIN ENTRY--PERSONAL NAME | |
| Personal name | Menna Allah Mohamed Ahmed Abdelmageed |
| 245 10 - TITLE STATEMENT | |
| Title | Design and synthesis of some fused pyrimidine derivatives with potential activity against cancer kinome / |
| Statement of responsibility, etc. | Menna Allah Mohamed Ahmed Abdelmageed ; Supervised Amal Abdelhaleem Mohamed Eissa , Awatef Elsaid Farag , Essam Eldin Abdelfattah Osman |
| 246 15 - VARYING FORM OF TITLE | |
| Title proper/short title | تصميم وتشييد بعض مشتقات البيريميدين الملتحمة ذات فاعلية محتملة على كينوم السرطان |
| 260 ## - PUBLICATION, DISTRIBUTION, ETC. | |
| Place of publication, distribution, etc. | Cairo : |
| Name of publisher, distributor, etc. | Menna Allah Mohamed Ahmed Abdelmageed , |
| Date of publication, distribution, etc. | 2021 |
| 300 ## - PHYSICAL DESCRIPTION | |
| Extent | 178 P. : |
| Other physical details | charts ; |
| Dimensions | 25cm |
| 502 ## - DISSERTATION NOTE | |
| Dissertation note | Thesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry |
| 520 ## - SUMMARY, ETC. | |
| Summary, etc. | Novel furan VIa-c, furo[2,3-d]pyrimidine VIIa-f, IX, Xa-f, XIIa,c, XIVa-d and furo[3,2-e][1,2,4]triazolo[1,5-c]pyrimidine VIIIa-f derivatives were designed based on their structural similarity to a previously described oxazole VEGFR-2 back pocket binding fragment.The twenty-eight designed compounds were synthesized and screened for their in vitro VEGFR-2 inhibitory activity where they exhibited good to moderate nanomolar inhibition with improved ligand efficiencies. VIIIb and Xc (IC₅₀ = 38.72 ± 1.7 and 41.40 ± 1.8 nM, respectively) were equipotent to sorafenib and VIa, VIc, VIIf, VIIIa, VIIIc, Xb, Xf, XIIc, XIVc and XIVd showed good activity (IC₅₀ = 43.31-98.31 nM). Additionally, all the novel compounds were evaluated for their antiproliferative activity at the National Cancer Institute (NCI), USA using sulforhodamine B assay (SRB) at a single dose of 10 oM and compounds XIVa,b were selected for NCI-60 five-dose screen to determine their Growth inhibition 50% (GI50), total growth inhibition (TGI) and lethal concentration 50% (LC50).The furotriazolopyrimidines VIIIa-c and furopyrimidine derivative Xc were further evaluated for their in vitro antiproliferative activity against human umbilical vein endothelial cells (HUVECs) where VIIIb showed higher potency than sorafenib and resulted in cell cycle arrest at G2/M phase whereas VIIIc revealed good antiproliferative activity with cell cycle arrest at G1 phase. Moreover, VIIIa-c and Xc showed significant inhibitory effects on the invasion and migration of HUVECs. Molecular docking study was conducted to gain insight about the potential binding mode. The furo[3,2-e][1,2,4]triazolo[1,5-c]pyrimidine derivatives VIIIb and VIIIc among the synthesized compounds represent interesting starting point for antiangiogenic compounds based on their activity and favorable drug likeness profiles |
| 530 ## - ADDITIONAL PHYSICAL FORM AVAILABLE NOTE | |
| Additional physical form available note | Issued also as CD |
| 653 #4 - INDEX TERM--UNCONTROLLED | |
| Uncontrolled term | Cancer kinome |
| 653 #4 - INDEX TERM--UNCONTROLLED | |
| Uncontrolled term | Design |
| 653 #4 - INDEX TERM--UNCONTROLLED | |
| Uncontrolled term | Fused pyrimidine |
| 700 0# - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Amal Abdelhaleem Mohamed Eissa , |
| Relator term | |
| 700 0# - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Awatef Elsaid Farag , |
| Relator term | |
| 700 0# - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Essam Eldin Abdelfattah Osman , |
| 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.Me.D | 01010110085212000 | 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.Me.D | 01020110085212000 | 22.09.2023 | CD - Rom | 85212.CD |