Executive Summary : | The indolo[2,3-a]carbazole ring system are present in many natural products and are regarded as the “privileged structure” for drug discovery, these scaffolds with simple and flexible synthetic transformations allow the production of large chemical libraries to generate potent bioactive molecules. Tjipanozole alkaloids having indolo [2,3-a] carbazole ring system have exhibited important biological activities such as cytotoxic activity against a panel of human tumor cell lines, antituberculosis, antimalarial activity and antibiotics can bind to DNA, antihuman cytomegalovirus (HCMV), potent cross-species microRNA inhibitors. Some naturally occurring and pharmaceutically important indolo[2,3-a] carbazole drugs are Flinderoles, isoborreverine, Rebeccamycin, Tjipanazole, and Staurosporine. Due to their structure complexity and impressive biological activity the PI has interest to make tjipanazoles and its analogues by a short synthesis pathway. Furthermore, small modification on these scaffolds can have surprising effects on target specificity. In fact, synthetic and medicinal chemistry studies provide many types semi-synthetic derivatives, which some have progressed through various phases of human clinical trials (eg. CEP-701, UCN-01). So, the present proposal is made to design and develop a good number of tjipanazole analogues for possible anticancer agents. |