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العنوان
Synthesis of certain substituted benzothiophene derivatives aspotential anticancer agents /
الناشر
Shimaa Magdy Ibrahim Alhamaky ,
المؤلف
Shimaa Magdy Ibrahim Alhamaky
هيئة الاعداد
باحث / Shimaa Magdy Ibrahim Alhamaky
مشرف / Nadia Abdalla Khalil
مشرف / Eman Mohamed Ahmed
مشرف / Ashraf Fouad Zaher
تاريخ النشر
2021
عدد الصفحات
164 P. :
اللغة
الإنجليزية
الدرجة
الدكتوراه
التخصص
العلوم الصيدلية
تاريخ الإجازة
4/10/2020
مكان الإجازة
جامعة القاهرة - كلية الصيدلة - Organic Chemistry
الفهرس
Only 14 pages are availabe for public view

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from 190

Abstract

Thesis comprises four chapters: The first chapter is an introduction which is composed of two parts.The first, is a brief literature survey on the synthesis of benzo[b]thiophen-3(2H)-ones, thioaurones, 4H-benzo[4,5]thieno[3,2-b]pyrans and pyranopyrimidine derivatives. The second part highlights theanticancer activity of some reported benzothiophene derivatives.The second chapter demonstrates the aim of the work, the rational of designing of the new target compounds with potential anticancer activity acting through inhibition of topoisomerase I enzyme, along with the proposed Schemes (1-3) detailing the pathways used for the preparation of the target compounds. In Scheme 1,a series of the key intermediate chalcones,IIa-fwas prepared via the reaction ofbenzo[b]thiophen-3(2H)-onesIa or Ib with the appropriate aromatic aldehydes in acetic acid containing anhydrous sodium acetate.Scheme2, includesthecyclization of IIa-fto the corresponding benzothienopyrans IIIa-f and IVa-f by the reactionwith active methylene containing compounds such as malononitrileor ethyl cyanoacetate,respectively. Scheme 3, describes the formation of compounds Va-f, VIa-f and VIIa-f.Reaction of compoundsIIIa-fwith p-chlorobenzaldehyde in dry toluene and with triethyl orthoformate in acetic anhydride afforded compoundsVa-f andVIa-f, respectively. Further, reaction of the latter with n-propylamine in ethanol gave compoundsVIIa-f. Third chapter consists of theoretical discussion of the experimental work followed for the preparation of the new compounds, and interpretation of their spectroscopic data