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Synthesis of some new pyrazoles and their fused derivatives as antitumor agents /

Emad Abdullah Deeb

Synthesis of some new pyrazoles and their fused derivatives as antitumor agents / تشييد بعض البيرازولات الجديدة ومشتقاتها الملتحمة كمضادات للأورام Emad Abdullah Deeb ; Supervised Nadia Hanafy Metwally - Cairo : Emad Abdullah Deeb , 2018 - 200 P. : charts ; 25cm

Thesis (Ph.D.) - Cairo University - Faculty of Science - Department of Organic Chemistry

The original work of this thesis includes: The key intermediate 3-aminopyrazolo[4,3-c]pyridine-4,6-dione (2) is considered as a precursor for some novel pyrazolo[4,3-c]pyridines such as 5a-c, 6a-c, arylhydrazopyrazolo[4,3-c]-pyridines 8a-e pyrazolo[4,5,1-ij][1,6] naphthyridines 11a-e, 18a-d and pyrido[4',3':3,4]pyrazolo[1,5-a]-pyrimidines 15a-d, 19a-p through Knovenegal condensation, coupling reaction and Michael addition. The structures were confirmed by elemental analyses, spectral data and all possible have been postulated to account for their formation. Some of the newly synthesized pyrazolo[4,3-c]pyridine derivatives were investigated for anticancer activity. The results of the cytotoxic activity revealed that compound 6b was the most active compound against the breast and liver carcinoma cell lines which gives IC50 values of 1.937 and 3.695 æg/mL, respectively compared to reference drug (doxorubicin) with IC50 values of 2.527 and 4.749 æg/ml, respectively



3-Aminopyrazolo [4,3-c]-pyridine-4,6-dione 3-Cyanomethyl-4-cyano-5-amino-1H-pyrazole Pyrazolo[4,3-c]pyridines