Design, synthesis and biological screening of novel quinazoline and pyrrolotriazine derivatives as potent HER-2 and VEGFR-2 inhibitors / (Record no. 81122)
[ view plain ]
| 000 -LEADER | |
|---|---|
| fixed length control field | 03085cam a2200349 a 4500 |
| 003 - CONTROL NUMBER IDENTIFIER | |
| control field | EG-GiCUC |
| 005 - DATE AND TIME OF LATEST TRANSACTION | |
| control field | 20250223032743.0 |
| 008 - FIXED-LENGTH DATA ELEMENTS--GENERAL INFORMATION | |
| fixed length control field | 210531s2021 ua dh 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.Ta.D |
| 100 0# - MAIN ENTRY--PERSONAL NAME | |
| Personal name | Tamer Abdellatif Abdelrhman Elwaie |
| 245 10 - TITLE STATEMENT | |
| Title | Design, synthesis and biological screening of novel quinazoline and pyrrolotriazine derivatives as potent HER-2 and VEGFR-2 inhibitors / |
| Statement of responsibility, etc. | Tamer Abdellatif Abdelrhman Elwaie ; Supervised Safinaz E. Abbas , Riham F. George , Hamed Ismail Ali |
| 246 15 - VARYING FORM OF TITLE | |
| Title proper/short title | VEGFR2 وال HER-2 تصميم وتشييد ومسح بيولوجى لمشتقات جديدة من الكينازولين والبيرولوتريازين كمثبطات فعالة لل |
| 260 ## - PUBLICATION, DISTRIBUTION, ETC. | |
| Place of publication, distribution, etc. | Cairo : |
| Name of publisher, distributor, etc. | Tamer Abdellatif Abdelrhman Elwaie , |
| Date of publication, distribution, etc. | 2021 |
| 300 ## - PHYSICAL DESCRIPTION | |
| Extent | 215 P. : |
| Other physical details | charts , facsimiles ; |
| Dimensions | 25cm |
| 502 ## - DISSERTATION NOTE | |
| Dissertation note | Thesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry |
| 520 ## - SUMMARY, ETC. | |
| Summary, etc. | Quinazoline and pyrrolotriazine are interesting bioactive scaffolds that elicit a wide range of biological activities including anticancer activity. According to WHO Global Cancer Country Profiles, breast and liver cancers are the most prevalent cancers worldwide. Herein, we highlighted on the anticancer activity of the quinazoline and pyrrolotriazine nuclei as protein tyrosine kinase inhibitors. HER-2 and VEGFR2 kinases as well-established targets for breast cancer (BC) and liver cancer (HCC) therapy, respectively, are associated with aggressive clinical outcomes.Thus, the present investigation deals with design and synthesis of a new series of twenty seven quinazoline derivatives (72a-c, 77a-l, 79a-d and 87a-h) and twenty pyrrolotriazine derivatives (102a-j, 103a-e and 107a-e), as lapatinib and sorafenib congeners, respectively, aiming to identify new alternative drug candidates for treatment of breast and liver cancers.The newly synthesized compounds were screened for their enzyme inhibitory and anticancer activities.The results revealed that, the developed quinazoline derivatives demonstrated potent HER-2 inhibitions (IC₅₀: 5.4{u2212}12 nM) compared to lapatinib (IC50: 95.5 nM), significant selective and potent antiproliferative activities ({u223C}20-fold) against HER-2+ (AU565, BT474) compared to HER-2({u2212})cells. Favorably, the quinazoline derivative(79d)exhibited potent in vivo tumor regression against the BT474 xenograft model with high metabolic stability and low intrinsic clearance (T1/2 > 145 min and CLint(mic) < 9.6 mL/min/kg) |
| 530 ## - ADDITIONAL PHYSICAL FORM AVAILABLE NOTE | |
| Additional physical form available note | Issued also as CD |
| 653 #4 - INDEX TERM--UNCONTROLLED | |
| Uncontrolled term | Human Epidermal Growth Factor Receptor 2. (HER-2) |
| 653 #4 - INDEX TERM--UNCONTROLLED | |
| Uncontrolled term | Pyrrolotriazine |
| 653 #4 - INDEX TERM--UNCONTROLLED | |
| Uncontrolled term | Quinazoline |
| 700 0# - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Hamed Ismail Ali , |
| Relator term | |
| 700 0# - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Riham F. George , |
| Relator term | |
| 700 0# - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Safinaz E. Abbas , |
| 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.Ta.D | 01010110083557000 | 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.Ta.D | 01020110083557000 | 22.09.2023 | CD - Rom | 83557.CD |