Synthesis of novel oxadiazole and chromene derivatives as cytotoxic agents / Nehal Mohamed Nabil Elbakhshawangy ; Supervised Azza Taher Taher Shalaby , Hala Bakr Ali Elnassan , Asmaa Elsayed Abdellatief Kassab
Material type:
TextLanguage: English Publication details: Cairo : Nehal Mohamed Nabil Elbakhshawangy , 2018Description: 140 P. : charts ; 25cmOther title: - تشييد مشتقات جديدة من الأوكساديازول و الكرومين كمضادات للأورام [Added title page title]
- Issued also as CD
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Thesis
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قاعة الرسائل الجامعية - الدور الاول | المكتبة المركزبة الجديدة - جامعة القاهرة | Cai01.08.04.M.Sc.2018.Ne.S (Browse shelf(Opens below)) | Not for loan | 01010110076992000 | ||
CD - Rom
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مخـــزن الرســائل الجـــامعية - البدروم | المكتبة المركزبة الجديدة - جامعة القاهرة | Cai01.08.04.M.Sc.2018.Ne.S (Browse shelf(Opens below)) | 76992.CD | Not for loan | 01020110076992000 |
Thesis (M.Sc.) - Cairo University - Faculty of Pharmacy - Department of Organic Chemistry
The design and synthesis of 1,3,4-oxadiazoles and chromenopyrimidines as microtubule destabilizing agents has been explained. The newly synthesized compounds were evaluated for their cytotoxicity against MCF-7 cell line. All the prepared chromenopyrimidines showed potent cytotoxic activity. Compound XVb was the leading compound as it showed IC₅₀ values of 0.13 oM on tumor cell line MCF-7 (11-fold more active than the reference drug colchicine) and 14.06 oM on mammary epithelial cell line MCF-10A. Also, it inhibited tubulin polymerization (IC₅₀ = 8.36oM), caused cell cycle arrest at G2/M phase (five folds more than control) and cellular apoptosis. Moreover, it increased the level of active caspase-3, 12-fold compared with control.
Issued also as CD
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