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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.