Nehal Mohamed Nabil Elbakhshawangy <br/><br/>
Synthesis of novel oxadiazole and chromene derivatives as cytotoxic agents /  
 تشييد مشتقات جديدة من الأوكساديازول و الكرومين كمضادات للأورام 
Nehal Mohamed Nabil Elbakhshawangy ; Supervised Azza Taher Taher Shalaby , Hala Bakr Ali Elnassan , Asmaa Elsayed Abdellatief Kassab 
 - Cairo :   Nehal Mohamed Nabil Elbakhshawangy ,   2018 
 - 140 P. :   charts ;   25cm  
<br/><br/>Thesis (M.Sc.) - Cairo University - Faculty of Pharmacy - Department of Organic Chemistry 
<br/><br/> 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. 
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<br/><br/><label>Subjects--Index Terms: </label>Chromene derivatives Cytotoxic agents Novel oxadiazole