Basic Informations

C.V

Name:
Rania Badawy Bakr Mohamed.
Languages spoken and written:
Arabic and English.
Current Address:
Birthday
Department of Pharmaceutical organic chemistry, Faculty of Pharmacy, Beni Suef University,
Beni Suef, Egypt.
Tel. 082 2332468 (home) 082 2319397 (work) 01004842863 (mobile)
Fax. 082 2317958
Email: raniabakr@ymail.com
rania.mohamed@pharm.bsu.edu.eg

Master Title

Synthesis of heterocyclic compounds of biological effect

Master Abstract

This thesis comprises four chapters. The first one is an introduction which consists of a brief survey on the different methods to synthesize pyrazolo[3,4-d]- pyrimidine containing compounds and their anticancer activity. The second chapter deals with the aim of the work and Schemes that have been carried out to obtain the new required pyrazolo[3,4-d]pyrimidine derivatives. The third chapter clarifies the theoretical discussion of the experimental work for the preparation of the starting materials Ia&b, IIa&b, Va&b and VIa&b, the new intermediate III which cyclized to pyrazolo[3,4-d]pyrimidinones IVa&b and the key intermediates VIIa-e and its acid hydrazide derivative VIII. In addition to the target new compounds IXa-e, Xa-c, XIa&b, XIIa&b, XIIIa&b, XIVa&b, XVa-c, XVIa&b, XVIIa-c, XVIII, XIXa-d, XXa-d and Mannich bases XXIa-d. The structure elucidation of the new compounds was supported by element analysis, IR, 1H-NMR in addition to mass spectral data. Additionally, a brief account on the docking study was explained through the binding conformations in comparison with the cytotoxic results. The fourth chapter consists of the experimental part of this work which contains the detailed procedures used for the synthesis of the starting materials Ia&b, IIa&b, Va&b and VIa&b and the new pyrazolo[3,4-d]pyrimidine compounds III , IVa&b, VIIae- XXIa-d. In addition, data obtained from the element and spectral analyses as well as their physical properties are given in this chapter. It also sheds the light on the anticancer activity of ten compounds of newly synthesized derivatives compared with doxorubicin as a standard cytotoxic agent. Compound XIIIb exhibited the highest cytotoxic activity with IC50 10.39 µM. This chapter also clarifies the correlation between the results of molecular docking and the anticancer activity

PHD Title

Synthesis of some pyrazolo[3,4-d]pyrimidine derivatives of biological effect

PHD Abstract

four chapters. The first one is an introduction which comprises a brief survey on the different methods to synthesize pyrazolo[3,4-d]- pyrimidine compounds and their anticancer activity. The second chapter deals with the aim of the work and schemes that have been carried out to obtain the new required pyrazolo[3,4-d]pyrimidine derivatives. The third chapter clarifies the discussion of the experimental work for the preparation of the starting materials I and II and the newly synthesized compounds. Compound II was hydrolyzed to afford pyrazole-4-carboxylic acid III which was cyclized through the reaction with acetic anhydride to afford pyrazolo[3,4-d][1,3]oxazin-4-one IV. In addition, compounds V, VI, VIIa-e and VIIIa-c were synthesized from the reaction of pyrazolo[1,3]oxazin-4-one IV with phenylhydrazine, hydroxylamine hydrochloride, different aromatic amines and the appropriate amide or thioamide, sequentially. Reacting the oxazinone derivative IV with hydrazine hydrate afforded 5-amino derivative IX which was condensed with some aromatic aldehydes, certain acid anhydrides, pyrazolo[3,4-d][1,3]oxazin-4-one derivative IV and urea or thiourea to afford compounds Xa-e, XIa,b, XII and XIIIa,b, respectively. On the other hand, reacting IX with chloroacetyl chloride gave XIV. Cyclization of XIV with ammonium acetate and ammonium thiocyanate yielded pyrazolopyrimidotriazine XV and thiazolidinone XVI, respectively. Compound XIV was subjected to nucleophilic substitution reactions with different aromatic amines and two pyrimidothiones XVIIIa,b to afford compounds XVIIa-c and XIXa,b, respectively.