Thesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry

In a search for new anticancer candidates, and motivated by the pivotal role of class III histone deacetylase (Sirtuins) in the occurrence and development of a variety of diseases including cancer, in addition to the promising anticancer activity exhibited by SIRT2 inhibitors, it deemed of interest to design and synthesize new series of phenolic azomethine derivatives and 5-arylidene thiazolidinones as novel anticancer SIRT2 inhibitors. In this regards, docking studies were performed to support the implemented design strategies. The synthesized target compounds were subjected to SITR2 enzyme inhibitory assay. Additionally, in vitro cytotoxic activities of the targeted compounds were tested in the NCI-60 human tumor cell line anticancer drug screening program, subsequently their selective cytotoxicity against the lung cancer cell line HOP-92 and the brain cancer cell line SNB-75 was assayed. Furthermore, the most active compounds were then tested for their effect on the cell cycle and apoptotic induction activity, in addition to their growth inhibitory activity against the human normal lung fibroblast cell line WI-38

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