Design, synthesis and biological evaluation of novel quinazoline hybrids of anticipated anticancer activity / (رقم التسجيلة. 179779)
[ عرض عادي ]
| 000 -LEADER | |
|---|---|
| fixed length control field | 04677namaa22004451i 4500 |
| 003 - CONTROL NUMBER IDENTIFIER | |
| control field | EG-GICUC |
| 005 - أخر تعامل مع التسجيلة | |
| control field | 20260428103132.0 |
| 008 - FIXED-LENGTH DATA ELEMENTS--GENERAL INFORMATION | |
| fixed length control field | 260428s2025 |||a|||frm||| 000 0 eng d |
| 040 ## - CATALOGING SOURCE | |
| Original cataloguing agency | EG-GICUC |
| Language of cataloging | eng |
| Transcribing agency | EG-GICUC |
| Modifying agency | EG-GICUC |
| Description conventions | rda |
| 041 0# - LANGUAGE CODE | |
| Language code of text/sound track or separate title | eng |
| Language code of summary or abstract | eng |
| -- | ara |
| 049 ## - Acquisition Source | |
| Acquisition Source | Deposit |
| 082 04 - DEWEY DECIMAL CLASSIFICATION NUMBER | |
| Classification number | 615.19 |
| 092 ## - LOCALLY ASSIGNED DEWEY CALL NUMBER (OCLC) | |
| Classification number | 615.19 |
| Edition number | 21 |
| 097 ## - Degree | |
| Degree | M.Sc |
| 099 ## - LOCAL FREE-TEXT CALL NUMBER (OCLC) | |
| Local Call Number | Cai01.08.05.M.Sc.2025.Sh.D |
| 100 0# - MAIN ENTRY--PERSONAL NAME | |
| Authority record control number or standard number | Shahinaz Ali Mekawy Sayed, |
| Preparation | preparation. |
| 245 10 - TITLE STATEMENT | |
| Title | Design, synthesis and biological evaluation of novel quinazoline hybrids of anticipated anticancer activity / |
| Statement of responsibility, etc. | by Shahinaz Ali Mekawy Sayed ; Supervision Prof. Dr. Safinaz El-Sayed Abbas, Prof. Dr. Reem Khidr Arafa, Dr. Ahmed Khaled Ben Al-Waleid Farouk. |
| 246 15 - VARYING FORM OF TITLE | |
| Title proper/short title | تصميم وتشييد وتقييم بيولوجي لمركبات جديدة من الكينازولين المتوقع لها نشاط مضاد للسرطان |
| 264 #0 - PRODUCTION, PUBLICATION, DISTRIBUTION, MANUFACTURE, AND COPYRIGHT NOTICE | |
| Date of production, publication, distribution, manufacture, or copyright notice | 2025. |
| 300 ## - PHYSICAL DESCRIPTION | |
| Extent | 90 pages : |
| Other physical details | illustrations ; |
| Dimensions | 25 cm. + |
| Accompanying material | CD. |
| 336 ## - CONTENT TYPE | |
| Content type term | text |
| Source | rda content |
| 337 ## - MEDIA TYPE | |
| Media type term | Unmediated |
| Source | rdamedia |
| 338 ## - CARRIER TYPE | |
| Carrier type term | volume |
| Source | rdacarrier |
| 502 ## - DISSERTATION NOTE | |
| Dissertation note | Thesis (M.Sc)-Cairo University, 2025. |
| 504 ## - BIBLIOGRAPHY, ETC. NOTE | |
| Bibliography, etc. note | Bibliography: pages 81-90. |
| 520 #3 - SUMMARY, ETC. | |
| Summary, etc. | Eighteen compounds of 6-nitro-4-substituted quinazolines IVa-c, VIIa-c, Xa-e and XIIa-d along with the 6-amino analogues Va,Vb and VIII have been synthesized and evaluated for their VEGFR-2 inhibition. The majority of the tested compounds displayed significant inhibition, where IVa, XIc and XIe displayed the most potent enzyme inhibition. The cytotoxic estimation of these compounds on HepG2, MCF-7 and HCT-116 cancer cell lines revealed the outstanding cytotoxicity of XIc on HepG2 and HCT-116 relative to sorafenib, in addition to their safety towards WI-38 normal cells. Also, compound XIc was found to cause cell cycle arrest at G1 phase and apoptotic induction, along with an increase in Bax /Bcl2 ratio in HepG2 cells, in addition to inhibition of wound closure. Molecular docking of IVa, XIc and XIe in VEGFR-2 active site revealed their binding modes, whereas dynamic simulation of XIc ensured its stability and dynamic behavior in VEGFR-2 binding site. |
| 520 #3 - SUMMARY, ETC. | |
| Summary, etc. | تم تشييد وتقييم ثمانية عشر مركبا من ال -6 نيترو- -4مستبدل الكينازولين IVa-c، VIIa-c، XIa-e و XIIIa-d بالإضافة إلي النظائر من ال 6-أمينو قد تم تشييدهم وتقييمهم كمثبطات لإنزيم VEGFR-2. وقد أظهرت غالبية المركبات نشاطا تثبيطيا ملحوظا حيث كانت المركبات IVa, XIc, XIe أكثر فعالية كمثبطات للإنزيم . وعند اختبار السمية الخلوية لهذه المركبات معمليا علي خطوط الخلايا السرطانية HCT-116 (خلايا سرطان القولون) و MCF-7 (خلية سرطان الصدر) و HepG2 (خلية سرطان الكبد ) وجد أن للمركب XIc نشاطا مميزا علي خطوط خلايا ال HCT-116 و HepG2 مقارنة بال sorafenib بالإضافة إلي درجة أمان عالية ضد الخلايا الطبيعية WI-38 . و قد وجد أن المركب XIc يسبب توقف في دورة خلايا الكبد HepG2 عند المرحلة G1 بالإضافة إلي إحداث موت مبرمج للخلية. كما أظهر المركب XIc ارتفاعا في نسبة ال Bax/Bcl-2 بالأضافة إلي تثبيط إلتئام الجروح وقد أظهرت النمذجة الجزيئية للمركبات IVa, XIc, XIe في الموقع النشط لإنزيم ال VEGFR-2 درجة ترابطهم مع الإنزيم ، بينما أكدت المحاكاة الديناميكية للمركب XIc مدي ثبات المركب والسلوك الديناميكي له في موقع الربط لإنزيم ال VEGFR-2 . |
| 530 ## - ADDITIONAL PHYSICAL FORM AVAILABLE NOTE | |
| Issues CD | Issues also as CD. |
| 546 ## - LANGUAGE NOTE | |
| Text Language | Text in English and abstract in Arabic & English. |
| 650 #0 - SUBJECT ADDED ENTRY--TOPICAL TERM | |
| Topical term or geographic name entry element | Pharmaceutical Chemistry |
| 650 #0 - SUBJECT ADDED ENTRY--TOPICAL TERM | |
| Topical term or geographic name entry element | كيمياء صيدلية |
| 653 #1 - INDEX TERM--UNCONTROLLED | |
| Uncontrolled term | Quinazolines |
| -- | VEGFR-2 |
| -- | Cytotoxicity |
| -- | Sorafenib |
| -- | HepG2 |
| -- | Molecular docking |
| -- | Molecular dynamic |
| -- | كينازولين |
| -- | السمية الخلوية |
| 700 0# - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Safinaz El-Sayed Abbas |
| Relator term | thesis advisor. |
| 700 0# - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Reem Khidr Arafa |
| Relator term | thesis advisor. |
| 700 0# - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Ahmed Khaled Ben Al-Waleid Farouk |
| Relator term | thesis advisor. |
| 900 ## - Thesis Information | |
| Grant date | 01-01-2025 |
| Supervisory body | Safinaz El-Sayed Abbas |
| -- | Reem Khidr Arafa |
| -- | Ahmed Khaled Ben Al-Waleid Farouk |
| Universities | Cairo University |
| Faculties | Faculty of Pharmacy |
| Department | Department of Pharmaceutical Chemistry |
| 905 ## - Cataloger and Reviser Names | |
| Cataloger Name | Shimaa |
| 942 ## - ADDED ENTRY ELEMENTS (KOHA) | |
| Source of classification or shelving scheme | Dewey Decimal Classification |
| Koha item type | Thesis |
| Edition | 21 |
| Suppress in OPAC | No |
| Source of classification or shelving scheme | Home library | Current library | Date acquired | Inventory number | Full call number | Barcode | Date last seen | Effective from | Koha item type |
|---|---|---|---|---|---|---|---|---|---|
| Dewey Decimal Classification | المكتبة المركزبة الجديدة - جامعة القاهرة | قاعة الرسائل الجامعية - الدور الاول | 28.04.2026 | 93884 | Cai01.08.05.M.Sc.2025.Sh.D | 01010110093884000 | 28.04.2026 | 28.04.2026 | Thesis |