Synthesis, Molecular Docking, and Biological Activity Study of Some Unsaturated Carbonyl Derivatives Containing N and/or S Elements / (Record no. 166768)
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| 000 -LEADER | |
|---|---|
| fixed length control field | 05381namaa22004331i 4500 |
| 003 - CONTROL NUMBER IDENTIFIER | |
| control field | OSt |
| 005 - أخر تعامل مع التسجيلة | |
| control field | 20250223033236.0 |
| 008 - FIXED-LENGTH DATA ELEMENTS--GENERAL INFORMATION | |
| fixed length control field | 240422s2023 |||a|||fr|m|| 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 |
| Language code of sung or spoken text | ara |
| 049 ## - Acquisition Source | |
| Acquisition Source | Deposit |
| 082 04 - DEWEY DECIMAL CLASSIFICATION NUMBER | |
| Classification number | 572 |
| 092 ## - LOCALLY ASSIGNED DEWEY CALL NUMBER (OCLC) | |
| Classification number | 572 |
| Edition number | 21 |
| 097 ## - Degree | |
| Degree | M.Sc |
| 099 ## - LOCAL FREE-TEXT CALL NUMBER (OCLC) | |
| Local Call Number | Cai01.12.02.M.Sc.2023.Mo.S |
| 100 0# - MAIN ENTRY--PERSONAL NAME | |
| Authority record control number or standard number | Mona Mahmoud Ali Bekheet, |
| Preparation | preparation. |
| 245 10 - TITLE STATEMENT | |
| Title | Synthesis, Molecular Docking, and Biological Activity Study of Some Unsaturated Carbonyl Derivatives Containing N and/or S Elements / |
| Statement of responsibility, etc. | Presented by Mona Mahmoud Ali Bekheet; supervisors: Prof. Dr. Ismail Abdelshafy Abdelhamid, Dr. Mohamed Attia Ragheb, Dr. Marwa Hasan Soliman. |
| 246 15 - VARYING FORM OF TITLE | |
| Title proper/short title | التحضير و التنميط الجزيئي ودراسة النشاط البيولوجي لبعض مشتقات الكربونيل غير المشبعة المحتوية على عناصر النيتروجين و/أو الكبريت |
| 264 #0 - PRODUCTION, PUBLICATION, DISTRIBUTION, MANUFACTURE, AND COPYRIGHT NOTICE | |
| Date of production, publication, distribution, manufacture, or copyright notice | 2023. |
| 300 ## - PHYSICAL DESCRIPTION | |
| Extent | 118 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, 2023. |
| 504 ## - BIBLIOGRAPHY, ETC. NOTE | |
| Bibliography, etc. note | Bibliography: pages 95-118. |
| 520 ## - SUMMARY, ETC. | |
| Summary, etc. | Five novel cyanoacrylamides incorporating sulphamethoxazole (5-9) were synthesized and characterized by various spectral analysis tools. The antiproliferative properties of the synthesized derivatives towards three human cancer cell lines (HCT116, MDA-MB-231 and A549) have been evaluated using MTT viability assay. Compound 9, incorporating 4-(piperidin-1-yl)phenyl moiety, showed the highest potency against the three cell lines compared to doxorubicin. Flow cytometric analysis revealed that compound 9 could effectively induce apoptosis and cell cycle arrest at the S phase in HCT116 cells. Compound 9 could also suppress the migration of HCT116 cells in wound healing assay. The mechanistic studies suggested that compound 9 exerted its anticancer activity through inducing HCT116 cells apoptosis by up-regulating Bax and caspase-3, down-regulating Bcl2 and survivin, blocking cell cycle in the S phase by downregulating cyclin A1, and inhibiting migration by upregulating CDH1. Using UV-Vis and EB-displacement measurements, compound 9 could interact with CT-DNA through a moderate intercalative mode. Moreover, the molecular docking confirmed that compound 9 had good binding affinities toward the active site of different proteins (Bcl2, CDK2 and CDH1). In summary, 9 is introduced as a promising antitumor lead candidate that is worthy of further drug efficacy improvement and preclinical studies. . |
| 520 ## - SUMMARY, ETC. | |
| Summary, etc. | هذا العمل يتضمن تصنيع سلسلة جديدة من مركبات cyanoacrylamide المرتبطة ب sulphamethoxazole عبر تفاعل Knoevenagel condensation الذي يتضمن تفاعل aldehydes و sulphamethoxazole في حمض الأسيتيك في وجود أسيتات الصوديوم. في هذه الدراسة ، تم تصنيع سلسلة جديدة من cyanoacrylamide المرتبطة بمشتقات sulphamethoxazole (5-9) وتقييمها كعوامل قوية مضادة للسرطان ضد مجموعة من خطوط الخلايا السرطانية (MDA-MB-231 و A549 و HCT116). وقد لوحظ أن المركب (9)المحتوى على 4-(piperidin-1-yl)phenyl moiety اكثرهم نشاطاً ضد الخلايا السرطانية ، منع تكاثر خط الخلايا HCT116 بفاعلية أفضل مقارنة با doxorubicin. وجد أن (9) يسبب موت الخلايا وتوقف دورة الخلية في المرحلة S في خلايا HCT116. أيضًا ، قام المركب (9) بتقليل cell migration بشكل كبير. علاوة على ذلك ، قام المركب (9) بزيادة تصنيع البروتينات المحفزة لعمليه apoptosis مثل Bax و CDH1 و caspase-3 ، بينما تم تقليل تصنيع Bcl2 و survivin و cyclin A1 بشكل كبير. أيضًا ، أظهرت جميع المركبات ، ولا سيما (5) و (9) ، photocleavage activity ضد DNA pBR322 البلازميد. يُظهر المركب (9) قدرة intercalating with CT-DNA باستخدام UV-Vis و EB quenching measurements. ، و من خلال الدراسه النظريه Docking Studies اثبتت ان المركب (9) له قدرة عاليه على الإرتباط ببعض البروتينات مثل Bcl2 و Cdk2و CDH1 وتشير هذه الدراسة إلى أن المركب (9) قد يكون له القدرة على العمل كدواء لعلاج سرطان القولون |
| 530 ## - ADDITIONAL PHYSICAL FORM AVAILABLE NOTE | |
| Issues CD | Issued also as CD |
| 546 ## - LANGUAGE NOTE | |
| Text Language | Text in English and abstract in Arabic & English. |
| 650 #7 - SUBJECT ADDED ENTRY--TOPICAL TERM | |
| Topical term or geographic name entry element | Biochemistry |
| Source of heading or term | qmark |
| 653 #0 - INDEX TERM--UNCONTROLLED | |
| Uncontrolled term | Cyanoacrylamide |
| -- | Antiproliferative activity |
| -- | Apoptosis |
| -- | Cell cycle arrest |
| -- | Docking |
| -- | DNA binding |
| 700 0# - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Ismail Abdelshafy Abdelhamid |
| Relator term | thesis advisor. |
| 700 0# - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Mohamed Attia Ragheb |
| Relator term | thesis advisor. |
| 700 0# - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Marwa Hasan Soliman |
| Relator term | thesis advisor. |
| 900 ## - Thesis Information | |
| Grant date | 01-01-2023 |
| Supervisory body | Ismail Abdelshafy Abdelhamid |
| -- | Mohamed Attia Ragheb |
| -- | Marwa Hasan Soliman |
| Universities | Cairo University |
| Faculties | Faculty of Science |
| Department | Department of Biochemistry |
| 905 ## - Cataloger and Reviser Names | |
| Cataloger Name | Huda |
| 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 | 22.04.2024 | 88247 | Cai01.12.02.M.Sc.2023.Mo.S | 01010110088247000 | 22.04.2024 | 22.04.2024 | Thesis |