Bishoy Y A El-Aarag
Menofia University, Egypt
Title: Novel phthalimide analogs as anti-angiogenic and anti-cancer agents
Biography
Biography: Bishoy Y A El-Aarag
Abstract
Phthalimide moiety is one of thalidomide metabolites and might be the effective part of thalidomide toward many diseases. The mode of action of thalidomide in cancer therapy mainly depends on its immunomodulatory and anti-angiogenic activity, therefore, the current study focused on the efficacy of the newly synthesized phthalimide derivatives as immunostimulatory/immunosuppressive agents against immune cells, and their growth inhibitory effect against various cancer cell lines, as well as their anti-angiogenic activity. A facile synthetic approach of novel phthalimide dithiocarbamate and dithioate analogs 4a-k, 5a-e and 5g-k was achieved by the reaction of N-chloromethyl or N-bromoethylphthalimide with carbon disulfide (CS2) and different amines. Phthalimide derivatives 5e and 5i exhibited the highest cytotoxic activities against MCF-7 and Hep-G2 cells. Both derivatives 5e and 5i inhibited nitric oxide (NO), tumor necrosis factor-α (TNF-α), vessel endothelial growth factor (VEGF) and its receptor (VEGFR). Derivative 5e showed immunosuppressive activity through its inhibition of immune cell functions and proliferation. Taken together, our study improved that some of the newly synthesized phthalimide derivatives may act as anti-angiogenic and anti-cancer agents