Design synthesis and biological evaluation of novel isatin derivatives as potential anti cancer agents / Hany Said Ibrahim ; Supervised Sahar Mahmoud AbouSeri , Hatem Abdelkader Abdelaziz

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

The discovery of efficacious new therapeutic agents is one of humanity's most vital tasks as health is one of the most important domains that human beings have focused on. Nowadays, we have a large number of cancer types that are widely spread and affect human health. Although, there is a large number of clinically used antitumor drugs, yet there is no cancer treatment that is 100% effective against disseminated cancer. Therefore, there is an urgent need to give much attention to update and modify drug leads from the point of view of medicinal chemistry and drug design to fulfil more potent and effective therapies. The reported antitumor activity of certain isatin derivatives has led to an increasing demand for the synthesis of new derivatives of anticipated antitumor activity. Accordingly, the present investigation deals with the synthesis of 3 - hydrazinoindolin - 2 - one derivatives that target cancer cells via two different mechanisms namely, inhibition of tumor-associated carbonic anhydrase and induction of apoptosis. These mechanisms were confirmed through biological evaluation. The structures of the prepared compounds were confirmed using various spectroscopic tools (IR, 1H NMR, 13C NMR, and mass spectra) as well as elemental analyses and single crystal X - ray crystallography

Issued also as CD