The original work of the present book consists of three research projects: In the first part: Synthesis, cytotoxicity evaluation, molecular docking and utility of novel chalcones as precursors for heterocycles incorporating pyrazole moiety.In the second part: Synthesis and antimicrobial activity of novel azolopyrimidines and pyrido-triazolo-pyrimidinones incorporating pyrazole moiety.In the third part: Synthesis of new pyrazolyl-pyridines as antitumor agents. The assigned structures for all the newly synthesized compounds were confirmed on the basis of elemental analyses and spectral data and the mechanisms of their formation were also discussed. In addition, some of the newly synthesized chalcones were tested for their cytotoxicity against human colon carcinoma cell line (HCT-116) and against human hepatocellular carcinoma (HEPG2) cell lines and the results revealed that some compounds have promising activities compared with the standard drug Doxorubicin. Molecular docking was also carried out for the high potent compounds.
This work has been carried out to investigate the following: The first project represents the reactions of ethylidenethiosemicarbazone with DMAD or substituted methylenemalononitriles gave thiazolidin-4-one or 1,3-thiazine derivatives, respectively. Also, treatment of ethylidenethiosemicarbazide with hydrazonoyl halides, -haloketones, and chloroacetic acid afforded the corresponding arylazothiazoles, thiazoles, and thiazolidenone derivative, respectively. The anti-cancer activity of the selected products against the colon carcinoma cell line (HCT-116) was determined and the results revealed promising activity.The second project involves the synthesis of a novel series of pyridine and bipyridine derivatives is described via one-pot multi-component reaction of 5-acetylimidazole, malononitrile (or ethyl cyanoacetate or diethyl malonate), substituted benzaldehyde (or terephthaldehyde) and ammonium acetate in good yields. The antimicrobial activities of the synthesized compounds were screened and the results showed that most of them exhibit considerable activities. Also, some of the newly synthesized compounds were screened for their anticancer activity against two cell lines.